Original:Mertansine 139504-50-0 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: Mertansine refers to the thiol-containing maytansinoid, DM1 (N2’-deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine) attached to a monoclonal antibody through reaction of the thiol group with the SPP (N-succinimidyl 4-(2-pyridyldithio)) linker to create an antibody-drug conjugate or ADC. Experimental ADCs with the SPP-DM1 design include lorvotuzumab mertansine. DM1 can also be linked to an antibody using the SMCC (4-(3-mercapto-2,5-dioxo-1-pyrrolidinylmethyl)-cylohexanecarboxylic acid) linker, in which case the International Nonproprietary Name of the conjugate formed contains the word emtansine. DM1 and its attachment via these linkers result from ImmunoGen Inc research. Trastuzumab emtansine (T-DM1) is an anti-HER2/neu antibody-drug conjugate.

Name: Mertansine (DM1) 

CAS#: 139504-50-0 

Chemical Formula: C35H48ClN3O10S 

Exact Mass: 737.27489 

Molecular Weight: 738.29 

Elemental Analysis: C, 56.94; H, 6.55; Cl, 4.80; N, 5.69; O, 21.67; S, 4.34

Synonym: DM1; DM-1; DM 1; DM1 Compound; DM1 [Maytansinoid]; Maytansinoid DM 1; Maytansinoid DM1; Maytansinoid DM-1; UNII-DDZ29HGH0E; maytansine, Mertansine; emtansine;

IUPAC/Chemical Name: (14S,16S,33S,2R,4R,10E,12Z,14R)-86-chloro-14-hydroxy-85,14-dimethoxy-33,2,7,10-tetramethyl-12,6-dioxo-7-aza-1(6,4)-oxazinana-3(2,3)-oxirana-8(1,3)-benzenacyclotetradecaphane-10,12-dien-4-yl N-(3-mercaptopropanoyl)-N-methyl-L-alaninate

InChi Key: ANZJBCHSOXCCRQ-GCRZMMRQSA-N

InChi Code: InChI=1S/C35H48ClN3O10S/c1-19-10-9-11-26(46-8)35(44)18-25(47-33(43)37-35)20(2)31-34(4,49-31)27(48-32(42)21(3)38(5)28(40)12-13-50)17-29(41)39(6)23-15-22(14-19)16-24(45-7)30(23)36/h9-11,15-16,20-21,25-27,31,44,50H,12-14,17-18H2,1-8H3,(H,37,43)/b11-9-,19-10+/t20-,21+,25+,26-,27-,31?,34+,35+/m1/s1

SMILES Code: C[C@@H]1[C@@H]2C[C@]([C@@H](/C=C\C=C(\CC3=CC(=C(C(=C3)OC)Cl)N(C(=O)C[C@H]([C@]4(C1O4)C)OC(=O)[C@H](C)N(C)C(=O)CCS)C)/C)OC)(NC(=O)O2)O

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

REFERENCES

1: Koniev O, Kolodych S, Baatarkhuu Z, Stojko J, Eberova J, Bonnefoy JY, Cianférani S, Van Dorsselaer A, Wagner A. MAPN: First-in-Class Reagent for Kinetically Resolved Thiol-to-Thiol Conjugation. Bioconjug Chem. 2015 Sep 3. [Epub ahead of print] PubMed PMID: 26335849.

2: Van den Mooter T, Teuwen LA, Rutten A, Dirix L. Trastuzumab emtansine in advanced human epidermal growth factor receptor 2-positive breast cancer. Expert Opin Biol Ther. 2015 May;15(5):749-60. doi: 10.1517/14712598.2015.1036026. PubMed PMID: 25865453.

3: Loganzo F, Tan X, Sung M, Jin G, Myers JS, Melamud E, Wang F, Diesl V, Follettie MT, Musto S, Lam MH, Hu W, Charati MB, Khandke K, Kim KS, Cinque M, Lucas J, Graziani E, Maderna A, O'Donnell CJ, Arndt KT, Gerber HP. Tumor cells chronically treated with a trastuzumab-maytansinoid antibody-drug conjugate develop varied resistance mechanisms but respond to alternate treatments. Mol Cancer Ther. 2015 Apr;14(4):952-63. doi: 10.1158/1535-7163.MCT-14-0862. Epub 2015 Feb 2. PubMed PMID: 25646013.

4: Robak T, Robak E. Current Phase II antibody-drug conjugates for the treatment of lymphoid malignancies. Expert Opin Investig Drugs. 2014 Jul;23(7):911-24. doi: 10.1517/13543784.2014.908184. Epub 2014 Apr 7. Review. PubMed PMID: 24708159.

5: Whiteman KR, Johnson HA, Mayo MF, Audette CA, Carrigan CN, LaBelle A, Zukerberg L, Lambert JM, Lutz RJ. Lorvotuzumab mertansine, a CD56-targeting antibody-drug conjugate with potent antitumor activity against small cell lung cancer in human xenograft models. MAbs. 2014 Mar-Apr;6(2):556-66. doi: 10.4161/mabs.27756. Epub 2014 Jan 8. PubMed PMID: 24492307; PubMed Central PMCID: PMC3984343.

6: Berdeja JG. Lorvotuzumab mertansine: antibody-drug-conjugate for CD56+ multiple myeloma. Front Biosci (Landmark Ed). 2014 Jan 1;19:163-70. Review. PubMed PMID: 24389179.

7: Patel TA, Dave B, Rodriguez AA, Chang JC, Perez EA, Colon-Otero G. Dual HER2 blockade: preclinical and clinical data. Breast Cancer Res. 2014 Aug 1;16(4):419. doi: 10.1186/s13058-014-0419-5. Erratum in: Breast Cancer Res. 2014;16(6):468. PubMed PMID: 25928889; PubMed Central PMCID: PMC4429364.

8: Wood AC, Maris JM, Gorlick R, Kolb EA, Keir ST, Reynolds CP, Kang MH, Wu J, Kurmasheva RT, Whiteman K, Houghton PJ, Smith MA. Initial testing (Stage 1) of the antibody-maytansinoid conjugate, IMGN901 (Lorvotuzumab mertansine), by the pediatric preclinical testing program. Pediatr Blood Cancer. 2013 Nov;60(11):1860-7. doi: 10.1002/pbc.24647. Epub 2013 Jun 24. PubMed PMID: 23798344; PubMed Central PMCID: PMC4260400.

9: van de Donk NW, Lokhorst HM. New developments in the management and treatment of newly diagnosed and relapsed/refractory multiple myeloma patients. Expert Opin Pharmacother. 2013 Aug;14(12):1569-73. doi: 10.1517/14656566.2013.805746. Epub 2013 May 31. PubMed PMID: 23721099.

10: Ballantyne A, Dhillon S. Trastuzumab emtansine: first global approval. Drugs. 2013 May;73(7):755-65. doi: 10.1007/s40265-013-0050-2. Review. PubMed PMID: 23620199.

11: Pode-Shakked N, Shukrun R, Mark-Danieli M, Tsvetkov P, Bahar S, Pri-Chen S, Goldstein RS, Rom-Gross E, Mor Y, Fridman E, Meir K, Simon A, Magister M, Kaminski N, Goldmacher VS, Harari-Steinberg O, Dekel B. The isolation and characterization of renal cancer initiating cells from human Wilms' tumour xenografts unveils new therapeutic targets. EMBO Mol Med. 2013 Jan;5(1):18-37. doi: 10.1002/emmm.201201516. Epub 2012 Dec 13. PubMed PMID: 23239665; PubMed Central PMCID: PMC3569651.

12: Lambert JM. Drug-conjugated antibodies for the treatment of cancer. Br J Clin Pharmacol. 2013 Aug;76(2):248-62. doi: 10.1111/bcp.12044. Review. PubMed PMID: 23173552; PubMed Central PMCID: PMC3731599.

13: Beck A, Lambert J, Sun M, Lin K. Fourth World Antibody-Drug Conjugate Summit: February 29-March 1, 2012, Frankfurt, Germany. MAbs. 2012 Nov-Dec;4(6):637-47. doi: 10.4161/mabs.21697. Epub 2012 Aug 22. PubMed PMID: 22909934; PubMed Central PMCID: PMC3502230.

14: Erickson HK, Lambert JM. ADME of antibody-maytansinoid conjugates. AAPS J. 2012 Dec;14(4):799-805. doi: 10.1208/s12248-012-9386-x. Epub 2012 Aug 9. Review. PubMed PMID: 22875610; PubMed Central PMCID: PMC3475867.

15: Gurtner K, Hessel F, Eicheler W, Dörfler A, Zips D, Heider KH, Krause M, Baumann M. Combined treatment of the immunoconjugate bivatuzumab mertansine and fractionated irradiation improves local tumour control in vivo. Radiother Oncol. 2012 Mar;102(3):444-9. doi: 10.1016/j.radonc.2011.10.013. Epub 2011 Nov 17. PubMed PMID: 22100655.

16: Ricart AD. Immunoconjugates against solid tumors: mind the gap. Clin Pharmacol Ther. 2011 Apr;89(4):513-23. doi: 10.1038/clpt.2011.8. Epub 2011 Mar 2. Review. PubMed PMID: 21368753.

17: Platt VM, Szoka FC Jr. Anticancer therapeutics: targeting macromolecules and nanocarriers to hyaluronan or CD44, a hyaluronan receptor. Mol Pharm. 2008 Jul-Aug;5(4):474-86. doi: 10.1021/mp800024g. Epub 2008 Jun 3. Review. PubMed PMID: 18547053; PubMed Central PMCID: PMC2772999.

18: Rodon J, Garrison M, Hammond LA, de Bono J, Smith L, Forero L, Hao D, Takimoto C, Lambert JM, Pandite L, Howard M, Xie H, Tolcher AW. Cantuzumab mertansine in a three-times a week schedule: a phase I and pharmacokinetic study. Cancer Chemother Pharmacol. 2008 Oct;62(5):911-9. doi: 10.1007/s00280-007-0672-8. Epub 2008 Feb 27. PubMed PMID: 18301896.

19: Riechelmann H, Sauter A, Golze W, Hanft G, Schroen C, Hoermann K, Erhardt T, Gronau S. Phase I trial with the CD44v6-targeting immunoconjugate bivatuzumab mertansine in head and neck squamous cell carcinoma. Oral Oncol. 2008 Sep;44(9):823-9. doi: 10.1016/j.oraloncology.2007.10.009. Epub 2008 Jan 18. PubMed PMID: 18203652.

20: Rupp U, Schoendorf-Holland E, Eichbaum M, Schuetz F, Lauschner I, Schmidt P, Staab A, Hanft G, Huober J, Sinn HP, Sohn C, Schneeweiss A. Safety and pharmacokinetics of bivatuzumab mertansine in patients with CD44v6-positive metastatic breast cancer: final results of a phase I study. Anticancer Drugs. 2007 Apr;18(4):477-85. PubMed PMID: 17351401.

Original:Olmutinib free base1353550-13-6 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

  

Description: Olmutinib, also known as HM61713 and BI-1482694, is a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK). BTK is a member of the Tec family of non-receptor protein tyrosine kinases. BTK is mostly expressed in hematopoietic cells such as B cells, mast cells and macrophages. BTK plays key roles in multiple cell signaling pathways including B-Cell Receptor (BCR) and Fc receptor (FcR) signaling cascades and is an essential mediator not only in B-cell dependent but also in myeloid cell dependent inflammatory arthritis. HM71224 has been selected as a novel therapeutic agent for the treatment of autoimmune diseases such as RA.

Name: Olmutinib free base 

CAS#: 1353550-13-6 (free base) 

Chemical Formula: C26H26N6O2S 

Exact Mass: 486.18379 

Molecular Weight: 486.59 

Elemental Analysis: C, 64.18; H, 5.39; N, 17.27; O, 6.58; S, 6.59

Synonym: HM61713; HM 61713; HM-61713; BI 1482694; BI-1482694; BI1482694; Olmutinib.

IUPAC/Chemical Name: N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)thieno[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide

InChi Key: FDMQDKQUTRLUBU-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H26N6O2S/c1-3-23(33)27-19-5-4-6-21(17-19)34-25-24-22(11-16-35-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h3-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)

SMILES Code: C=CC(NC1=CC=CC(OC2=C3C(C=CS3)=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

Related CAS# 

1353550-13-6 (free base); 1842366-97-5 (HCl). 

1802181-20-9 (deleted CAS#)

Note: Olmutinib was previously mistakely cited as "HM71224". As of 9/12/2016, there are many vendor still cit 

  

  

REFERENCES

1: Park K, Han JY, Kim DW, Bazhenova LA, Ou SH, Pang YK, Hin HS, Juan O, Son J, Jänne P. 190TiP: ELUXA 1: Phase II study of BI 1482694 (HM61713) in patients (pts) with T790M-positive non-small cell lung cancer (NSCLC) after treatment with an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI). J Thorac Oncol. 2016 Apr;11(4 Suppl):S139. doi: 10.1016/S1556-0864(16)30299-4. Epub 2016 Apr 15. PubMed PMID: 27198328.

2: Park K, Lee JS, Han JY, Lee KH, Kim JH, Cho EK, Cho JY, Min YJ, Kim JS, Kim DW. 1300: Efficacy and safety of BI 1482694 (HM61713), an EGFR mutant-specific inhibitor, in T790M-positive NSCLC at the recommended phase II dose. J Thorac Oncol. 2016 Apr;11(4 Suppl):S113. doi: 10.1016/S1556-0864(16)30243-X. Epub 2016 Apr 15. PubMed PMID: 27198272.

3: Wang S, Cang S, Liu D. Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. J Hematol Oncol. 2016 Apr 12;9:34. doi: 10.1186/s13045-016-0268-z. Review. PubMed PMID: 27071706; PubMed Central PMCID: PMC4830020.

4: Tan CS, Cho BC, Soo RA. Next-generation epidermal growth factor receptor tyrosine kinase inhibitors in epidermal growth factor receptor -mutant non-small cell lung cancer. Lung Cancer. 2016 Mar;93:59-68. doi: 10.1016/j.lungcan.2016.01.003. Epub 2016 Jan 8. Review. PubMed PMID: 26898616.

5: Song HN, Jung KS, Yoo KH, Cho J, Lee JY, Lim SH, Kim HS, Sun JM, Lee SH, Ahn JS, Park K, Choi YL, Park W, Ahn MJ. Acquired C797S Mutation upon Treatment with a T790M-Specific Third-Generation EGFR Inhibitor (HM61713) in Non-Small Cell Lung Cancer. J Thorac Oncol. 2016 Apr;11(4):e45-7. doi: 10.1016/j.jtho.2015.12.093. Epub 2015 Dec 31. PubMed PMID: 26749488.

6: Pirker R. Third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer. Curr Opin Oncol. 2016 Mar;28(2):115-21. doi: 10.1097/CCO.0000000000000260. PubMed PMID: 26720671.

7: Ou SH, Soo RA. Dacomitinib in lung cancer: a "lost generation" EGFR tyrosine-kinase inhibitor from a bygone era? Drug Des Devel Ther. 2015 Oct 15;9:5641-53. doi: 10.2147/DDDT.S52787. eCollection 2015. Review. PubMed PMID: 26508839; PubMed Central PMCID: PMC4610796.

8: Tartarone A, Lerose R. Clinical approaches to treat patients with non-small cell lung cancer and epidermal growth factor receptor tyrosine kinase inhibitor acquired resistance. Ther Adv Respir Dis. 2015 Oct;9(5):242-50. doi: 10.1177/1753465815587820. Epub 2015 May 27. Review. PubMed PMID: 26016841.

9: Wang H, Guo R, Zhang L. [TKI Resistance for T790M Mutation]. Zhongguo Fei Ai Za Zhi. 2015 Apr;18(4):245-50. doi: 10.3779/j.issn.1009-3419.2015.04.10. Review. Chinese. PubMed PMID: 25936890.

10: Liao BC, Lin CC, Yang JC. Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer. Curr Opin Oncol. 2015 Mar;27(2):94-101. doi: 10.1097/CCO.0000000000000164. Review. PubMed PMID: 25611025.

11: Stinchcombe TE. Recent advances in the treatment of non-small cell and small cell lung cancer. F1000Prime Rep. 2014 Dec 1;6:117. doi: 10.12703/P6-117. eCollection 2014. Review. PubMed PMID: 25580271; PubMed Central PMCID: PMC4251418.

12: Steuer CE, Khuri FR, Ramalingam SS. The next generation of epidermal growth factor receptor tyrosine kinase inhibitors in the treatment of lung cancer. Cancer. 2015 Apr 15;121(8):E1-6. doi: 10.1002/cncr.29139. Epub 2014 Dec 17. Review. PubMed PMID: 25521095.

13: Peters S, Zimmermann S, Adjei AA. Oral epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: comparative pharmacokinetics and drug-drug interactions. Cancer Treat Rev. 2014 Sep;40(8):917-26. doi: 10.1016/j.ctrv.2014.06.010. Epub 2014 Jul 1. PubMed PMID: 25027951.

Original:LOXO-101 (ARRY-470) 1223403-58-4 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: Larotrectinib, also known as ARRY-470 and LOXO-101, is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons.

Name: LOXO-101 (ARRY-470) 

CAS#: 1223403-58-4 

Chemical Formula: C21H22F2N6O2 

Exact Mass: 428.17723 

Molecular Weight: 428.44 

Elemental Analysis: C, 58.87; H, 5.18; F, 8.87; N, 19.62; O, 7.47

Synonym: LOXO 101; LOXO-101; LOXO101; ARRY-470; ARRY470; ARRY 470; larotrectinib

IUPAC/Chemical Name: (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide

InChi Key: NYNZQNWKBKUAII-KBXCAEBGSA-N

InChi Code: InChI=1S/C21H22F2N6O2/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31)/t14-,18+/m0/s1

SMILES Code: O=C(N1CC[C@@H](C1)O)NC2=C3N=C(N4CCC[C@@H]4C5=CC(F)=CC=C5F)C=CN3N=C2

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

   

  

  

REFERENCES

Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang, Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors and their preparation and use in the treatment of diseases. WO2010048314 (2010).

Original:Original: SAG (Smo agonist) free base 912545-86-9, stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); sag antagonizes cyclopamine action at the Smo receptor. SAG potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM). SAG induces pathway activation independently of Ptch proteins. The Smoothened receptor (SMO) mediates signal transduction in the hedgehog pathway, which is implicated in normal development and carcinogenesis. SMO antagonists can suppress the growth of some tumours.

Name: SAG (Smo agonist) free base 

CAS#: 912545-86-9 (free base) 

Chemical Formula: C28H28ClN3OS 

Exact Mass: 489.16416 

Molecular Weight: 490.06 

Elemental Analysis: C, 68.63; H, 5.76; Cl, 7.23; N, 8.57; O, 3.26; S, 6.54

Related CAS #: 2095432-58-7 (HCl)   912545-86-9 (free base)    

Synonym: SAG; SAG free base; SAG (Smo agonist); SAG (cyclopamine antagonist);

IUPAC/Chemical Name: 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide

InChi Key: VFSUUTYAEQOIMW-YHBQERECSA-N

InChi Code: InChI=1S/C28H28ClN3OS/c1-30-22-9-11-23(12-10-22)32(28(33)27-26(29)24-7-2-3-8-25(24)34-27)18-19-5-4-6-21(17-19)20-13-15-31-16-14-20/h2-8,13-17,22-23,30H,9-12,18H2,1H3/t22-,23-

SMILES Code: O=C(C1=C(Cl)C2=CC=CC=C2S1)N([C@H]3CC[C@H](NC)CC3)CC4=CC=CC(C5=CC=NC=C5)=C4

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Original:Original: Sapanisertib (MLN0128) 1224844-38-5, stock more than 100g

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Description: Sapanisertib, also known as TAK-228, MLN0128 and INK128, is a TORC1/2 inhibitor, is also an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity. TORC1/2 inhibitor INK128 binds to and inhibits both TORC1 and TORC2 complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. TORC1 and 2 are upregulated in some tumors and play an important role in the PI3K/Akt/mTOR signaling pathway, which is frequently dysregulated in human cancers.

Name: Sapanisertib (MLN0128) 

CAS#: 1224844-38-5 

Chemical Formula: C15H15N7O 

Exact Mass: 309.1338 

Molecular Weight: 309.333 

Elemental Analysis: C, 58.24; H, 4.89; N, 31.70; O, 5.17

Synonym: TAK-228; TAK 228; TAK228; INK128; INK-128; INK 128; MLN0128; MLN 0128; MLN-0128; Sapanisertib.

IUPAC/Chemical Name: 3-(2-amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

InChi Key: GYLDXIAOMVERTK-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)

SMILES Code: NC1=C2C(N(C(C)C)N=C2C3=CC=C(OC(N)=N4)C4=C3)=NC=N1

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

NK128 is an orally-available, potent and selective TORC1/2 inhibitor. INK128 has demonstrated broad preclinical anti-tumor activity against a range of solid tumor types. Potent inhibition was observed in cell lines resistant to rapamycin and pan-PI3K inhibitors.  Unlike other drugs targeting this pathway, INK128 inhibits the kinase activity associated with both the TORC1 and TORC2 complexes of the mTOR kinase. This dual TORC1 and TORC2 activity differentiates INK128 from rapamycin and various related analogs, or rapalogs, which only interfere with TORC1 activity, allowing for feedback loops that may actually augment tumor growth. In contrast, inhibition of both TORC1 and TORC2 may allow for improved efficacy and ultimately greater therapeutic potential for patient benefit. (source: http://www.intellikine.com/pipeline/ink128.html). 

    

REFERENCES

1: Maiso P, Liu Y, Morgan B, Azab A, Ren P, Martin MB, Zhang Y, Liu Y, Sacco A, Ngo H, Azab F, Quang P, Rodig SJ, Lin CP, Roccaro A, Rommel C, Ghobrial IM. Defining the role of TORC1 and TORC2 in multiple myeloma. Blood. 2011 Nov 1. [Epub ahead of print] PubMed PMID: 22045983.