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2017年7月31日星期一

COA 31785-68-9

EOS Med Chem produce 31785-68-9  assay 99.2% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

2017 China CPHI: E1M35
EOS Med Chem, Medchem is Big
執大象,天下往,往而無害,安平泰
網址www.eosmedchem.com 
労働時間: Beijing Time 4:00AM~11:00PM
郵箱info@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp & Wechat: +8618653174435
住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian

2017年7月30日星期日

MIDOSTAURIN 120685-11-2 ,100g in stock

Midostaurin, also known as PKC-412, PKC-412A and CGP 41251; is a synthetic indolocarbazole multikinase inhibitor with potential antiangiogenic and antineoplastic activities. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.

2017 China CPHI: E1M35
EOS Med Chem, Medchem is Big
執大象,天下往,往而無害,安平泰
網址www.eosmedchem.com 
労働時間: Beijing Time 4:00AM~11:00PM
郵箱info@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp & Wechat: +8618653174435
住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian

Name: Midostaurin 
CAS#: 120685-11-2 
Chemical Formula: C35H30N4O4 
Exact Mass: 570.22671 
Molecular Weight: 570.6371 
Elemental Analysis: C, 73.67; H, 5.30; N, 9.82; O, 11.22

Synonym: PKC-412; PKC412; PKC 412; PKC412A; PKC-412A; PKC 412A; CGP41251; CGP 41251; CGP-41251; Midostaurin
IUPAC/Chemical Name: N-((5R,7R,8R,9S)-8-methoxy-9-methyl-16-oxo-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide
InChi Key: BMGQWWVMWDBQGC-IIFHNQTCSA-N
InChi Code: InChI=1S/C35H30N4O4/c1-35-32(42-3)25(37(2)34(41)19-11-5-4-6-12-19)17-26(43-35)38-23-15-9-7-13-20(23)28-29-22(18-36-33(29)40)27-21-14-8-10-16-24(21)39(35)31(27)30(28)38/h4-16,25-26,32H,17-18H2,1-3H3,(H,36,40)/t25-,26-,32-,35+/m1/s1
SMILES Code: C[C@@]12[C@H](OC)[C@H](N(C(C3=CC=CC=C3)=O)C)C[C@H](N4C5=CC=CC=C5C6=C7C(CNC7=O)=C8C9=CC=CC=C9N2C8=C64)O1

REFERENCES

1: Kawai M, Nakashima A, Kamada S, Kikkawa U. Midostaurin preferentially attenuates proliferation of triple-negative breast cancer cell lines through inhibition of Aurora kinase family. J Biomed Sci. 2015 Jul 4;22(1):48. doi: 10.1186/s12929-015-0150-2. PubMed PMID: 26141684; PubMed Central PMCID: PMC4491224.
2: Yan F, Shen N, Pang J, Molina JR, Yang P, Liu S. The DNA Methyltransferase DNMT1 and Tyrosine-Protein Kinase KIT Cooperatively Promote Resistance to 5-aza-2'-deoxycytidine (Decitabine) and Midostaurin (PKC412) in Lung Cancer Cell. J Biol Chem. 2015 Jun 17. pii: jbc.M114.633693. [Epub ahead of print] PubMed PMID: 26085088.
3: Mirza Z, Schulten HJ, Farsi HM, Al-Maghrabi JA, Gari MA, Chaudhary AG, Abuzenadah AM, Al-Qahtani MH, Karim S. Molecular interaction of a kinase inhibitor midostaurin with anticancer drug targets, S100A8 and EGFR: transcriptional profiling and molecular docking study for kidney cancer therapeutics. PLoS One. 2015 Mar 19;10(3):e0119765. doi: 10.1371/journal.pone.0119765. eCollection 2015. PubMed PMID: 25789858; PubMed Central PMCID: PMC4366044.
4: Cooper BW, Kindwall-Keller TL, Craig MD, Creger RJ, Hamadani M, Tse WW, Lazarus HM. A Phase I Study of Midostaurin and Azacitidine in Relapsed and Elderly AML Patients. Clin Lymphoma Myeloma Leuk. 2015 Jul;15(7):428-432.e2. doi: 10.1016/j.clml.2015.02.017. Epub 2015 Feb 16. PubMed PMID: 25776192; PubMed Central PMCID: PMC4484305.
5: Strati P, Kantarjian H, Ravandi F, Nazha A, Borthakur G, Daver N, Kadia T, Estrov Z, Garcia-Manero G, Konopleva M, Rajkhowa T, Durand M, Andreeff M, Levis M, Cortes J. Phase I/II trial of the combination of midostaurin (PKC412) and 5-azacytidine for patients with acute myeloid leukemia and myelodysplastic syndrome. Am J Hematol. 2015 Apr;90(4):276-81. doi: 10.1002/ajh.23924. Epub 2015 Mar 2. PubMed PMID: 25530214; PubMed Central PMCID: PMC4376596.
6: Xu X, Kreisel FH, Frater JL, Hassan A. Mast cell leukemia with prolonged survival on PKC412/midostaurin. Int J Clin Exp Pathol. 2014 May 15;7(6):3439-43. eCollection 2014. PubMed PMID: 25031773; PubMed Central PMCID: PMC4097263.
7: Dutreix C, Lorenzo S, Wang Y. Comparison of two endogenous biomarkers of CYP3A4 activity in a drug-drug interaction study between midostaurin and rifampicin. Eur J Clin Pharmacol. 2014 Aug;70(8):915-20. doi: 10.1007/s00228-014-1675-0. Epub 2014 May 21. PubMed PMID: 24839948; PubMed Central PMCID: PMC4088993.
8: Wolleschak D, Mack TS, Perner F, Frey S, Schnöder TM, Wagner MC, Höding C, Pils MC, Parkner A, Kliche S, Schraven B, Hebel K, Brunner-Weinzierl M, Ranjan S, Isermann B, Lipka DB, Fischer T, Heidel FH. Clinically relevant doses of FLT3-kinase inhibitors quizartinib and midostaurin do not impair T-cell reactivity and function. Haematologica. 2014 Jun;99(6):e90-3. doi: 10.3324/haematol.2014.104331. Epub 2014 Mar 14. PubMed PMID: 24633870; PubMed Central PMCID: PMC4040902.
9: Ramsingh G, Westervelt P, McBride A, Stockerl-Goldstein K, Vij R, Fiala M, Uy G, Cashen A, Dipersio JF, Abboud CN. Phase I study of cladribine, cytarabine, granulocyte colony stimulating factor (CLAG regimen) and midostaurin and all-trans retinoic acid in relapsed/refractory AML. Int J Hematol. 2014 Mar;99(3):272-8. doi: 10.1007/s12185-014-1503-4. Epub 2014 Feb 2. PubMed PMID: 24488798; PubMed Central PMCID: PMC4406413.
10: Bourget P, Amin A, Chandesris MO, Vidal F, Merlette C, Hirsch I, Cabaret L, Carvalhosa A, Mogenet A, Frenzel L, Damaj G, Lortholary O, Hermine O. Liquid chromatography-tandem mass spectrometry assay for therapeutic drug monitoring of the tyrosine kinase inhibitor, midostaurin, in plasma from patients with advanced systemic mastocytosis. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Jan 1;944:175-81. doi: 10.1016/j.jchromb.2013.11.003. Epub 2013 Nov 15. PubMed PMID: 24316764.
11: Dutreix C, Munarini F, Lorenzo S, Roesel J, Wang Y. Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers. Cancer Chemother Pharmacol. 2013 Dec;72(6):1223-34. doi: 10.1007/s00280-013-2287-6. Epub 2013 Oct 2. PubMed PMID: 24085261; PubMed Central PMCID: PMC3834177.
12: Williams CB, Kambhampati S, Fiskus W, Wick J, Dutreix C, Ganguly S, Aljitawi O, Reyes R, Fleming A, Abhyankar S, Bhalla KN, McGuirk JP. Preclinical and phase I results of decitabine in combination with midostaurin (PKC412) for newly diagnosed elderly or relapsed/refractory adult patients with acute myeloid leukemia. Pharmacotherapy. 2013 Dec;33(12):1341-52. doi: 10.1002/phar.1316. Epub 2013 Jun 24. PubMed PMID: 23798029.
13: Gleixner KV, Peter B, Blatt K, Suppan V, Reiter A, Radia D, Hadzijusufovic E, Valent P. Synergistic growth-inhibitory effects of ponatinib and midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V. Haematologica. 2013 Sep;98(9):1450-7. doi: 10.3324/haematol.2012.079202. Epub 2013 Mar 28. PubMed PMID: 23539538; PubMed Central PMCID: PMC3762103.
14: Stone RM, Fischer T, Paquette R, Schiller G, Schiffer CA, Ehninger G, Cortes J, Kantarjian HM, DeAngelo DJ, Huntsman-Labed A, Dutreix C, del Corral A, Giles F. Phase IB study of the FLT3 kinase inhibitor midostaurin with chemotherapy in younger newly diagnosed adult patients with acute myeloid leukemia. Leukemia. 2012 Sep;26(9):2061-8. doi: 10.1038/leu.2012.115. Epub 2012 Apr 27. PubMed PMID: 22627678; PubMed Central PMCID: PMC4118284.
15: del Corral A, Dutreix C, Huntsman-Labed A, Lorenzo S, Morganroth J, Harrell R, Wang Y. Midostaurin does not prolong cardiac repolarization defined in a thorough electrocardiogram trial in healthy volunteers. Cancer Chemother Pharmacol. 2012 May;69(5):1255-63. doi: 10.1007/s00280-012-1825-y. PubMed PMID: 22294470; PubMed Central PMCID: PMC3337405.
16: Fischer T, Stone RM, Deangelo DJ, Galinsky I, Estey E, Lanza C, Fox E, Ehninger G, Feldman EJ, Schiller GJ, Klimek VM, Nimer SD, Gilliland DG, Dutreix C, Huntsman-Labed A, Virkus J, Giles FJ. Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3. J Clin Oncol. 2010 Oct 1;28(28):4339-45. doi: 10.1200/JCO.2010.28.9678. Epub 2010 Aug 23. PubMed PMID: 20733134; PubMed Central PMCID: PMC4135183.
17: Huang YC, Shieh HR, Chen YJ. Midostaurin (PKC412) modulates differentiation and maturation of human myeloid dendritic cells. Toxicol In Vitro. 2010 Sep;24(6):1705-10. doi: 10.1016/j.tiv.2010.05.015. Epub 2010 May 26. PubMed PMID: 20685248.
18: Krauth MT, Mirkina I, Herrmann H, Baumgartner C, Kneidinger M, Valent P. Midostaurin (PKC412) inhibits immunoglobulin E-dependent activation and mediator release in human blood basophils and mast cells. Clin Exp Allergy. 2009 Nov;39(11):1711-20. doi: 10.1111/j.1365-2222.2009.03353.x. PubMed PMID: 19860818.
19: Huang YC, Chao DK, Clifford Chao KS, Chen YJ. Oral small-molecule tyrosine kinase inhibitor midostaurin (PKC412) inhibits growth and induces megakaryocytic differentiation in human leukemia cells. Toxicol In Vitro. 2009 Sep;23(6):979-85. doi: 10.1016/j.tiv.2009.06.027. Epub 2009 Jun 30. PubMed PMID: 19573588.
20: Yin OQ, Wang Y, Schran H. A mechanism-based population pharmacokinetic model for characterizing time-dependent pharmacokinetics of midostaurin and its metabolites in human subjects. Clin Pharmacokinet. 2008;47(12):807-16. doi: 10.2165/0003088-200847120-00005. PubMed PMID: 19026036.

STAUROSPORINE 62996-74-1, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok. 100g in stock

Staurosporine, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.


2017 China CPHI: E1M35
EOS Med Chem, Medchem is Big
執大象,天下往,往而無害,安平泰
網址www.eosmedchem.com 
労働時間: Beijing Time 4:00AM~11:00PM
郵箱info@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp & Wechat: +8618653174435
住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian

Name: Staurosporine 
CAS#: 62996-74-1 
Chemical Formula: C28H26N4O3 
Exact Mass: 466.20049 
Molecular Weight: 466.54 
Elemental Analysis: C, 72.09; H, 5.62; N, 12.01; O, 10.29

Synonym: AM-2282; AM2282; AM 2282; STS; Antibiotic 230; CGP 41251; CGP41251; CGP-41251; CCRIS 3272; Staurosporine; Staurosporin.
IUPAC/Chemical Name: (5S,6R,7R,9R)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-14-one
InChi Key: HKSZLNNOFSGOKW-FYTWVXJKSA-N
InChi Code: InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
SMILES Code: CO[C@@H]1[C@@H](C[C@@H]2N3C4=C(N(C5=CC=CC=C56)[C@@]1(C)O2)C6=C7CNC(C7=C4C8=CC=CC=C83)=O)NC

Ubrogepant CAS 1374248-77-7

Ubrogepant CAS 1374248-77-7, Sole supplier

Ubrogepant Intermediate 1375541-21-1
Ubrogepant Intermediate 1375470-88-4
Ubrogepant Intermediate 1375541-21-1
Ubrogepant Intermediate 1455358-14-1
Ubrogepant Intermediate 1455358-12-9
Ubrogepant Intermediate 1455358-11-8
Ubrogepant Intermediate 1375470-88-4
Ubrogepant Intermediate 1375477-14-7
Ubrogepant Intermediate 93267-04-0
Ubrogepant Intermediate 14123-60-5





2017 China CPHI: E1M35
EOS Med Chem, Medchem is Big
執大象,天下往,往而無害,安平泰
網址www.eosmedchem.com 
労働時間: Beijing Time 4:00AM~11:00PM
郵箱info@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp & Wechat: +8618653174435
住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian


Pralatrexate & Intermeidate 146464-93-9

Pralatrexate & Intermeidate 146464-93-9, EOS is China top supplier.

We keep 1-5kg in stock.

Assay HPLC 99.2%, NMR, HPLC, LCMS, MOA, MSDS, COA is ok.
www.eosmedchem.com


2017 China CPHI: E1M35
EOS Med Chem, Medchem is Big
執大象,天下往,往而無害,安平泰
網址: www.eosmedchem.com 
労働時間: Beijing Time 4:00AM~11:00PM
郵箱: info@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp & Wechat: +8618653174435
住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian






Pralatrexate is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities. Pralatrexate selectively enters cells expressing RFC-1; intracellularly, this agent is highly polyglutamylated and competes for the folate binding site of DHFR, blocking tetrahydrofolate synthesis, which may result in depletion of nucleotide precursors; inhibition of DNA, RNA and protein synthesis; and apoptotic tumor cell death.


Name: Pralatrexate 
CAS#: 146464-95-1 
Chemical Formula: C23H23N7O5 
Exact Mass: 477.17607 
Molecular Weight: 477.47 
Elemental Analysis: C, 57.86; H, 4.86; N, 20.53; O, 16.75


Synonym: Pralatrexate
IUPAC/Chemical Name: N -(4-{1-[(2,4-diaminopteridin-6-yl)methyl]but-3-yn-1-yl}benzoyl)-L-glutamic acid
InChi Key: OGSBUKJUDHAQEA-WMCAAGNKSA-N
InChi Code: InChI=1S/C23H23N7O5/c1-2-3-14(10-15-11-26-20-18(27-15)19(24)29-23(25)30-20)12-4-6-13(7-5-12)21(33)28-16(22(34)35)8-9-17(31)32/h1,4-7,11,14,16H,3,8-10H2,(H,28,33)(H,31,32)(H,34,35)(H4,24,25,26,29,30)/t14?,16-/m0/s1
SMILES Code: O=C(O)CC[C@@H](C(O)=O)NC(C1=CC=C(C(CC2=NC3=C(N)N=C(N)N=C3N=C2)CC#C)C=C1)=O

REFERENCES

1: Kelly KR, Gabrail N, Weitman S, Sarantopoulos J, Olszanski AJ, Edenfield W, Venitz J, Reddy G, Yang A, Hasal SJ, Lockhart AC. Phase 1 study evaluating the safety and pharmacokinetics of pralatrexate in relapsed/refractory advanced solid tumors and lymphoma patients with mild, moderate, and severe renal impairment. Cancer Chemother Pharmacol. 2016 Nov;78(5):929-939. PubMed PMID: 27638045.
2: Del Carmen MG, Supko JG, Horick NK, Rauh-Hain JA, Clark RM, Campos SM, Krasner CN, Atkinson T, Birrer MJ. Phase 1 and 2 study of carboplatin and pralatrexate in patients with recurrent, platinum-sensitive ovarian, fallopian tube, or primary peritoneal cancer. Cancer. 2016 Nov 15;122(21):3297-3306. doi: 10.1002/cncr.30196. PubMed PMID: 27421044.
3: Sastry RV, Venkatesan CS, Sastry BS, Mahesh K. Identification and characterization of forced degradation products of pralatrexate injection by LC-PDA and LC-MS. J Pharm Biomed Anal. 2016 Nov 30;131:400-409. doi: 10.1016/j.jpba.2016.08.023. PubMed PMID: 27643862.
4: Lee SS, Jung SH, Ahn JS, Kim YK, Cho MS, Jung SY, Lee JJ, Kim HJ, Yang DH. Pralatrexate in Combination with Bortezomib for Relapsed or Refractory Peripheral T Cell Lymphoma in 5 Elderly Patients. J Korean Med Sci. 2016 Jul;31(7):1160-3. doi: 10.3346/jkms.2016.31.7.1160. PubMed PMID: 27366017; PubMed Central PMCID: PMC4901011.
5: Dunn TJ, Dinner S, Price E, Coutré SE, Gotlib J, Hao Y, Berube C, Medeiros BC, Liedtke M. A phase 1, open-label, dose-escalation study of pralatrexate in combination with bortezomib in patients with relapsed/refractory multiple myeloma. Br J Haematol. 2016 Apr;173(2):253-9. doi: 10.1111/bjh.13946. PubMed PMID: 27040320.
6: McPherson JP, Vrontikis A, Sedillo C, Halwani AS, Gilreath JA. Pralatrexate Monitoring Using a Commercially Available Methotrexate Assay to Avoid Potential Drug Interactions. Pharmacotherapy. 2016 Feb;36(2):e8-e11. doi: 10.1002/phar.1699. PubMed PMID: 26809959.
7: Advani RH, Ansell SM, Lechowicz MJ, Beaven AW, Loberiza F, Carson KR, Evens AM, Foss F, Horwitz S, Pro B, Pinter-Brown LC, Smith SM, Shustov AR, Savage KJ, Vose JM. A phase II study of cyclophosphamide, etoposide, vincristine and prednisone (CEOP) Alternating with Pralatrexate (P) as front line therapy for patients with peripheral T-cell lymphoma (PTCL): final results from the T- cell consortium trial. Br J Haematol. 2016 Feb;172(4):535-44. doi: 10.1111/bjh.13855. PubMed PMID: 26627450.
8: Wood GS, Wu J. Methotrexate and Pralatrexate. Dermatol Clin. 2015 Oct;33(4):747-55. doi: 10.1016/j.det.2015.05.009. Review. PubMed PMID: 26433846.
9: Grem JL, Kos ME, Evande RE, Meza JL, Schwarz JK. A phase 1 clinical trial of sequential pralatrexate followed by a 48-hour infusion of 5-fluorouracil given every other week in adult patients with solid tumors. Cancer. 2015 Nov 1;121(21):3862-8. doi: 10.1002/cncr.29504. PubMed PMID: 26242208.
10: Petullo B, Wei L, Yereb M, Neal A, Rose J, Bekaii-Saab T, Wu C. A phase II study of biweekly pralatrexate and docetaxel in patients with advanced esophageal and gastroesophageal carcinoma that have failed first-line platinum-based therapy. J Gastrointest Oncol. 2015 Jun;6(3):336-40. doi: 10.3978/j.issn.2078-6891.2015.011. PubMed PMID: 26029462; PubMed Central PMCID: PMC4397239.
11: Tedeschi PM, Kathari YK, Johnson-Farley N, Bertino JR. Methylthioadenosine phosphorylase (MTAP)-deficient T-cell ALL xenografts are sensitive to pralatrexate and 6-thioguanine alone and in combination. Cancer Chemother Pharmacol. 2015 Jun;75(6):1247-52. doi: 10.1007/s00280-015-2747-2. PubMed PMID: 25917288; PubMed Central PMCID: PMC4441744.
12: Jain S, Jirau-Serrano X, Zullo KM, Scotto L, Palermo CF, Sastra SA, Olive KP, Cremers S, Thomas T, Wei Y, Zhang Y, Bhagat G, Amengual JE, Deng C, Karan C, Realubit R, Bates SE, O'Connor OA. Preclinical pharmacologic evaluation of pralatrexate and romidepsin confirms potent synergy of the combination in a murine model of human T-cell lymphoma. Clin Cancer Res. 2015 May 1;21(9):2096-106. doi: 10.1158/1078-0432.CCR-14-2249. PubMed PMID: 25677697.
13: Tedeschi PM, Kathari YK, Farooqi IN, Bertino JR. Leucovorin rescue allows effective high-dose pralatrexate treatment and an increase in therapeutic index in mesothelioma xenografts. Cancer Chemother Pharmacol. 2014 Nov;74(5):1029-32. doi: 10.1007/s00280-014-2580-z. PubMed PMID: 25205429; PubMed Central PMCID: PMC4209237.
14: A phase II study of cyclophosphamide, etoposide, vincristine and prednisone (CEOP) alternating with pralatrexate (P) as front line therapy for patients with peripheral T-cell lymphoma (PTCL): preliminary results from the T-Cell Consortium trial. Clin Adv Hematol Oncol. 2014 Feb;12(2 Suppl 5):6-7. PubMed PMID: 24852788.
15: Visentin M, Unal ES, Goldman ID. The impact of 5-formyltetrahydrofolate on the anti-tumor activity of pralatrexate, as compared to methotrexate, in HeLa cells in vitro. Cancer Chemother Pharmacol. 2014 May;73(5):1055-62. doi: 10.1007/s00280-014-2441-9. PubMed PMID: 24682532; PubMed Central PMCID: PMC4018754.
16: Dondi A, Bari A, Pozzi S, Ferri P, Sacchi S. The potential of pralatrexate as a treatment of peripheral T-cell lymphoma. Expert Opin Investig Drugs. 2014 May;23(5):711-8. doi: 10.1517/13543784.2014.902050. Review. PubMed PMID: 24661228.
17: Talpur R, Thompson A, Gangar P, Duvic M. Pralatrexate alone or in combination with bexarotene: long-term tolerability in relapsed/refractory mycosis fungoides. Clin Lymphoma Myeloma Leuk. 2014 Aug;14(4):297-304. doi: 10.1016/j.clml.2014.01.010. PubMed PMID: 24589156.
18: Ho AL, Lipson BL, Sherman EJ, Xiao H, Fury MG, Apollo A, Seetharamu N, Sima CS, Haque S, Lyo JK, Sales R, Cox L, Pfister DG. A phase II study of pralatrexate with vitamin B12 and folic acid supplementation for previously treated recurrent and/or metastatic head and neck squamous cell cancer. Invest New Drugs. 2014 Jun;32(3):549-54. doi: 10.1007/s10637-014-0073-x. PubMed PMID: 24566705.
19: Kerdel FA, Styperek AR, Maini A. Clinical remission of primary aggressive CD8+ cutaneous T-cell lymphoma after pralatrexate infusion. JAMA Dermatol. 2014 Mar;150(3):320-2. doi: 10.1001/jamadermatol.2013.8647. PubMed PMID: 24452280.
20: Marchi E, Mangone M, Zullo K, O'Connor OA. Pralatrexate pharmacology and clinical development. Clin Cancer Res. 2013 Dec 15;19(24):6657-61. doi: 10.1158/1078-0432.CCR-12-2251. PubMed PMID: 23965902.

2017年7月29日星期六

FLUTICASONE PROPIONATE INTERMEDIATE 80474-45-9

EOS Med Chem produce FLUTICASONE PROPIONATE INTERMEDIATE 80474-45-9  assay 99.2% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

2017 China CPHI: E1M35
EOS Med Chem, Medchem is Big
執大象,天下往,往而無害,安平泰
網址www.eosmedchem.com 
労働時間: Beijing Time 4:00AM~11:00PM
郵箱info@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp & Wechat: +8618653174435
住所: Diaozhen Chemical Industrial Park, Jinan City, China
Skype: willgutian
QQ: 2393923585


2017年7月28日星期五

Ribociclib key Intermediate 1211443-61-6

EOS Med Chem produce Ribociclib key Intermediate 1211443-61-6, assay 99.2% to be China biggest.
Ribociclib key Intermediate 1211443-61-6, assay 99.2% NMR, MS, COA is OK.
Ribociclib key Intermediate 1211443-61-6, assay 99.2% Size batch could be 100kg.

2017 China CPHI: E1M35
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2017年7月26日星期三

EOS Pralatrexate 146464-95-1

EOS Pralatrexate 146464-95-1


Pralatrexate is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities. Pralatrexate selectively enters cells expressing RFC-1; intracellularly, this agent is highly polyglutamylated and competes for the folate binding site of DHFR, blocking tetrahydrofolate synthesis, which may result in depletion of nucleotide precursors; inhibition of DNA, RNA and protein synthesis; and apoptotic tumor cell death.




Name: Pralatrexate 
CAS#: 146464-95-1 
Chemical Formula: C23H23N7O5 
Exact Mass: 477.17607 
Molecular Weight: 477.47 
Elemental Analysis: C, 57.86; H, 4.86; N, 20.53; O, 16.75

Synonym: Pralatrexate
IUPAC/Chemical Name: N -(4-{1-[(2,4-diaminopteridin-6-yl)methyl]but-3-yn-1-yl}benzoyl)-L-glutamic acid
InChi Key: OGSBUKJUDHAQEA-WMCAAGNKSA-N
InChi Code: InChI=1S/C23H23N7O5/c1-2-3-14(10-15-11-26-20-18(27-15)19(24)29-23(25)30-20)12-4-6-13(7-5-12)21(33)28-16(22(34)35)8-9-17(31)32/h1,4-7,11,14,16H,3,8-10H2,(H,28,33)(H,31,32)(H,34,35)(H4,24,25,26,29,30)/t14?,16-/m0/s1
SMILES Code: O=C(O)CC[C@@H](C(O)=O)NC(C1=CC=C(C(CC2=NC3=C(N)N=C(N)N=C3N=C2)CC#C)C=C1)=O

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2: Del Carmen MG, Supko JG, Horick NK, Rauh-Hain JA, Clark RM, Campos SM, Krasner CN, Atkinson T, Birrer MJ. Phase 1 and 2 study of carboplatin and pralatrexate in patients with recurrent, platinum-sensitive ovarian, fallopian tube, or primary peritoneal cancer. Cancer. 2016 Nov 15;122(21):3297-3306. doi: 10.1002/cncr.30196. PubMed PMID: 27421044.
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4: Lee SS, Jung SH, Ahn JS, Kim YK, Cho MS, Jung SY, Lee JJ, Kim HJ, Yang DH. Pralatrexate in Combination with Bortezomib for Relapsed or Refractory Peripheral T Cell Lymphoma in 5 Elderly Patients. J Korean Med Sci. 2016 Jul;31(7):1160-3. doi: 10.3346/jkms.2016.31.7.1160. PubMed PMID: 27366017; PubMed Central PMCID: PMC4901011.
5: Dunn TJ, Dinner S, Price E, Coutré SE, Gotlib J, Hao Y, Berube C, Medeiros BC, Liedtke M. A phase 1, open-label, dose-escalation study of pralatrexate in combination with bortezomib in patients with relapsed/refractory multiple myeloma. Br J Haematol. 2016 Apr;173(2):253-9. doi: 10.1111/bjh.13946. PubMed PMID: 27040320.
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8: Wood GS, Wu J. Methotrexate and Pralatrexate. Dermatol Clin. 2015 Oct;33(4):747-55. doi: 10.1016/j.det.2015.05.009. Review. PubMed PMID: 26433846.
9: Grem JL, Kos ME, Evande RE, Meza JL, Schwarz JK. A phase 1 clinical trial of sequential pralatrexate followed by a 48-hour infusion of 5-fluorouracil given every other week in adult patients with solid tumors. Cancer. 2015 Nov 1;121(21):3862-8. doi: 10.1002/cncr.29504. PubMed PMID: 26242208.
10: Petullo B, Wei L, Yereb M, Neal A, Rose J, Bekaii-Saab T, Wu C. A phase II study of biweekly pralatrexate and docetaxel in patients with advanced esophageal and gastroesophageal carcinoma that have failed first-line platinum-based therapy. J Gastrointest Oncol. 2015 Jun;6(3):336-40. doi: 10.3978/j.issn.2078-6891.2015.011. PubMed PMID: 26029462; PubMed Central PMCID: PMC4397239.
11: Tedeschi PM, Kathari YK, Johnson-Farley N, Bertino JR. Methylthioadenosine phosphorylase (MTAP)-deficient T-cell ALL xenografts are sensitive to pralatrexate and 6-thioguanine alone and in combination. Cancer Chemother Pharmacol. 2015 Jun;75(6):1247-52. doi: 10.1007/s00280-015-2747-2. PubMed PMID: 25917288; PubMed Central PMCID: PMC4441744.
12: Jain S, Jirau-Serrano X, Zullo KM, Scotto L, Palermo CF, Sastra SA, Olive KP, Cremers S, Thomas T, Wei Y, Zhang Y, Bhagat G, Amengual JE, Deng C, Karan C, Realubit R, Bates SE, O'Connor OA. Preclinical pharmacologic evaluation of pralatrexate and romidepsin confirms potent synergy of the combination in a murine model of human T-cell lymphoma. Clin Cancer Res. 2015 May 1;21(9):2096-106. doi: 10.1158/1078-0432.CCR-14-2249. PubMed PMID: 25677697.
13: Tedeschi PM, Kathari YK, Farooqi IN, Bertino JR. Leucovorin rescue allows effective high-dose pralatrexate treatment and an increase in therapeutic index in mesothelioma xenografts. Cancer Chemother Pharmacol. 2014 Nov;74(5):1029-32. doi: 10.1007/s00280-014-2580-z. PubMed PMID: 25205429; PubMed Central PMCID: PMC4209237.
14: A phase II study of cyclophosphamide, etoposide, vincristine and prednisone (CEOP) alternating with pralatrexate (P) as front line therapy for patients with peripheral T-cell lymphoma (PTCL): preliminary results from the T-Cell Consortium trial. Clin Adv Hematol Oncol. 2014 Feb;12(2 Suppl 5):6-7. PubMed PMID: 24852788.
15: Visentin M, Unal ES, Goldman ID. The impact of 5-formyltetrahydrofolate on the anti-tumor activity of pralatrexate, as compared to methotrexate, in HeLa cells in vitro. Cancer Chemother Pharmacol. 2014 May;73(5):1055-62. doi: 10.1007/s00280-014-2441-9. PubMed PMID: 24682532; PubMed Central PMCID: PMC4018754.
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17: Talpur R, Thompson A, Gangar P, Duvic M. Pralatrexate alone or in combination with bexarotene: long-term tolerability in relapsed/refractory mycosis fungoides. Clin Lymphoma Myeloma Leuk. 2014 Aug;14(4):297-304. doi: 10.1016/j.clml.2014.01.010. PubMed PMID: 24589156.
18: Ho AL, Lipson BL, Sherman EJ, Xiao H, Fury MG, Apollo A, Seetharamu N, Sima CS, Haque S, Lyo JK, Sales R, Cox L, Pfister DG. A phase II study of pralatrexate with vitamin B12 and folic acid supplementation for previously treated recurrent and/or metastatic head and neck squamous cell cancer. Invest New Drugs. 2014 Jun;32(3):549-54. doi: 10.1007/s10637-014-0073-x. PubMed PMID: 24566705.
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