TOP supplier: Eribulin Mesylate | 441045-17-6 and Intermediates

Eribulin Mesylate | 441045-17-6 API and Intermediates, 

we are one of China top supplier.

Until now, each Intermeidates, we could supply 1kg standard.

Eribulin  Intermediate CAS 157332-83-3;  Until 2017 May, we have more than 90g in stock, assay 98% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 1808153-90-3, Until 2017 May, we have more than 10g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 157322-47-9, Until 2017 May, we have more than 8g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 871360-12-2, Until 2017 May, we have more than 5g in stock, assay 99% in GMP plant, C-
GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 871348-22-0, Until 2017 May, we have more than 5g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 871348-24-2, Until 2017 May, we have more than 10g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 1808153-90-3, Until 2017 May, we have more than 15g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 1808153-90-3, Until 2017 May, we have more than 14g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 914922-88-6, Until 2017 May, we have more than 8g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin  Intermediate CAS 253128-10-8, Until 2017 May, we have more than 8g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin Intermediate CAS 253128-06-2, Until 2017 May, we have more than 40g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin Intermediate CAS 253128-15-3, Until 2017 May, we have more than 10g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.


Eribulin Intermediate CAS: 781360-42-8 , Until 2017 May, we have more than 10g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin Intermediate CAS:871360-43-9 , Until 2017 May, we have more than 10g in stock, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin raw materials: 1583253-09-1, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.


Eribulin raw materials:r 914922-88-6, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Eribulin raw materials: 1191256-09-3, 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

QQ: 2393923585

NMR, HPLC 99%, LCMS, Veliparib free base, CAS: 912444-00-9, 5G in stock, Pls check:

NMR, HPLC, LCMS, COA, Pls kindly check:

Description: Veliparib, also known as ABT-888, is a poly(ADP-ribose) polymerase (PARP) -1 and -2 inhibitor with chemosensitizing and antitumor activities. With no antiproliferative effects as a single agent at therapeutic concentrations, ABT-888 inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents.

Name: Veliparib free base 
CAS#: 912444-00-9 (free base) 
Chemical Formula: C13H16N4O 
Exact Mass: 244.13241 
Molecular Weight: 244.29 

Elemental Analysis: C, 63.91; H, 6.60; N, 22.93; O, 6.55

Related CAS #: 912444-00-9 (free base)   912445-05-7 (HCl)  
Synonym: ABT888; ABT-888; ABT 888; Veliparib
IUPAC/Chemical Name: (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide
InChi Key: JNAHVYVRKWKWKQ-CYBMUJFWSA-N
InChi Code: InChI=1S/C13H16N4O/c1-13(6-3-7-15-13)12-16-9-5-2-4-8(11(14)18)10(9)17-12/h2,4-5,15H,3,6-7H2,1H3,(H2,14,18)(H,16,17)/t13-/m1/s1


TECHNICAL DATA
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Certificate of Analysis:  View CoA: previous batch, Lot#BBC60321 
 View CoA: previous batch, Lot#TZC70327 
 View CoA: current batch, Lot#T7K08C22 
QC Data:  View QC data: previous batch, Lot#BBC60321 
 View QC data: previous batch, Lot#TZC70327 
 View QC data: current batch, Lot#T7K08C22 
Safety Data Sheet (MSDS):  View Material Safety Data Sheet (MSDS) 
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).

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

REFERENCES

1: Bhute VJ, Ma Y, Bao X, Palecek SP. The Poly (ADP-Ribose) Polymerase Inhibitor Veliparib and Radiation Cause Significant Cell Line Dependent Metabolic Changes in Breast Cancer Cells. Sci Rep. 2016 Nov 4;6:36061. doi: 10.1038/srep36061. PubMed PMID: 27811964; PubMed Central PMCID: PMC5095763.

2: Ramalingam SS, Blais N, Mazieres J, Reck M, Jones CM, Juhász E, Urban L, Orlov S, Barlési F, Kio E, Keiholz U, Qin Q, Qian J, Nickner C, Dziubinski J, Xiong H, Ansell P, McKee MD, Giranda V, Gorbunova V. Randomized, Placebo-Controlled, Phase 2 Study of Veliparib in Combination with Carboplatin and Paclitaxel for Advanced/Metastatic Non-Small Cell Lung Cancer. Clin Cancer Res. 2016 Oct 10. pii: clincanres.3069.2016. [Epub ahead of print] PubMed PMID: 27803064.

3: Munasinghe W, Stodtmann S, Tolcher A, Calvo E, Gordon M, Jalving M, de Vos-Geelen J, Medina D, Bergau D, Nuthalapati S, Hoffman D, Shepherd S, Xiong H. Effect of veliparib (ABT-888) on cardiac repolarization in patients with advanced solid tumors: a randomized, placebo-controlled crossover study. Cancer Chemother Pharmacol. 2016 Nov;78(5):1003-1011. PubMed PMID: 27709282; PubMed Central PMCID: PMC5083757.

4: Isakoff SJ, Puhalla S, Domchek SM, Friedlander M, Kaufman B, Robson M, Telli ML, Diéras V, Han HS, Garber JE, Johnson EF, Maag D, Qin Q, Giranda VL, Shepherd SP. A randomized Phase II study of veliparib with temozolomide or carboplatin/paclitaxel versus placebo with carboplatin/paclitaxel in BRCA1/2 metastatic breast cancer: design and rationale. Future Oncol. 2016 Oct 14. [Epub ahead of print] PubMed PMID: 27739325.

5: Chabot P, Hsia TC, Ryu JS, Gorbunova V, Belda-Iniesta C, Ball D, Kio E, Mehta M, Papp K, Qin Q, Qian J, Holen KD, Giranda V, Suh JH. Veliparib in combination with whole-brain radiation therapy for patients with brain metastases from non-small cell lung cancer: results of a randomized, global, placebo-controlled study. J Neurooncol. 2016 Sep 21. [Epub ahead of print] PubMed PMID: 27655223.

6: Subhash VV, Tan SH, Yeo MS, Yan FL, Peethala PC, Liem N, Krishnan V, Yong WP. ATM expression predicts Veliparib and Irinotecan sensitivity in gastric cancer by mediating P53 independent regulation of cell cycle and apoptosis. Mol Cancer Ther. 2016 Sep 16. pii: molcanther.1002.2015. [Epub ahead of print] PubMed PMID: 27638859.

7: Pratz KW, Rudek MA, Gojo I, Litzow MR, McDevitt MA, Ji JJ, Karnitz L, Herman JG, Kinders R, Smith BD, Gore SD, Carraway H, Showel MM, Gladstone DE, Levis MJ, Tsai HL, Rosner GL, Chen A, Kaufmann SH, Karp J. A Phase I study of topotecan, carboplatin and the PARP inhibitor veliparib in acute leukemias, aggressive myeloproliferative neoplasms and chronic myelomonocytic leukemia. Clin Cancer Res. 2016 Aug 22. pii: clincanres.1274.2016. [Epub ahead of print] PubMed PMID: 27551000.

8: Gojo I, Beumer JH, Pratz KW, McDevitt MA, Baer MR, Blackford AL, Smith BD, Gore SD, Carraway H, Showel MM, Levis MJ, Dezern A, Gladstone DE, Ji JJ, Wang L, Kinders R, Pouquet M, Ali-Walbi I, Rudek MA, Poh W, Herman JG, Karnitz L, Kaufmann SH, Chen A, Karp J. A phase 1 study of the PARP inhibitor veliparib in combination with temozolomide in acute myeloid leukemia. Clin Cancer Res. 2016 Aug 8. pii: clincanres.0984.2016. [Epub ahead of print] PubMed PMID: 27503200.

9: Rugo HS, Olopade OI, DeMichele A, Yau C, van 't Veer LJ, Buxton MB, Hogarth M, Hylton NM, Paoloni M, Perlmutter J, Symmans WF, Yee D, Chien AJ, Wallace AM, Kaplan HG, Boughey JC, Haddad TC, Albain KS, Liu MC, Isaacs C, Khan QJ, Lang JE, Viscusi RK, Pusztai L, Moulder SL, Chui SY, Kemmer KA, Elias AD, Edmiston KK, Euhus DM, Haley BB, Nanda R, Northfelt DW, Tripathy D, Wood WC, Ewing C, Schwab R, Lyandres J, Davis SE, Hirst GL, Sanil A, Berry DA, Esserman LJ; I-SPY 2 Investigators.. Adaptive Randomization of Veliparib-Carboplatin Treatment in Breast Cancer. N Engl J Med. 2016 Jul 7;375(1):23-34. doi: 10.1056/NEJMoa1513749. PubMed PMID: 27406347.

10: Kummar S, Wade JL, Oza AM, Sullivan D, Chen AP, Gandara DR, Ji J, Kinders RJ, Wang L, Allen D, Coyne GO, Steinberg SM, Doroshow JH. Randomized phase II trial of cyclophosphamide and the oral poly (ADP-ribose) polymerase inhibitor veliparib in patients with recurrent, advanced triple-negative breast cancer. Invest New Drugs. 2016 Jun;34(3):355-63. doi: 10.1007/s10637-016-0335-x. PubMed PMID: 26996385; PubMed Central PMCID: PMC4860030.

11: Villalona-Calero MA, Duan W, Zhao W, Shilo K, Schaaf LJ, Thurmond J, Westman JA, Marshall J, Xiaobai L, Ji J, Rose J, Lustberg M, Bekaii-Saab T, Chen A, Timmers C. Veliparib Alone or in Combination with Mitomycin C in Patients with Solid Tumors With Functional Deficiency in Homologous Recombination Repair. J Natl Cancer Inst. 2016 Feb 4;108(7). pii: djv437. doi: 10.1093/jnci/djv437. PubMed PMID: 26848151; PubMed Central PMCID: PMC4948564.

12: LoRusso PM, Li J, Burger A, Heilbrun LK, Sausville EA, Boerner SA, Smith D, Pilat MJ, Zhang J, Tolaney SM, Cleary JM, Chen AP, Rubinstein L, Boerner JL, Bowditch A, Cai D, Bell T, Wolanski A, Marrero AM, Zhang Y, Ji J, Ferry-Galow K, Kinders RJ, Parchment RE, Shapiro GI. Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor Veliparib (ABT-888) in Combination with Irinotecan in Patients with Advanced Solid Tumors. Clin Cancer Res. 2016 Jul 1;22(13):3227-37. doi: 10.1158/1078-0432.CCR-15-0652. PubMed PMID: 26842236; PubMed Central PMCID: PMC4930710.

13: Bogliolo S, Cassani C, Dominoni M, Musacchi V, Venturini PL, Spinillo A, Ferrero S, Gardella B. Veliparib for the treatment of ovarian cancer. Expert Opin Investig Drugs. 2016;25(3):367-74. doi: 10.1517/13543784.2016.1146677. Review. PubMed PMID: 26807493.

14: Rodler ET, Kurland BF, Griffin M, Gralow JR, Porter P, Yeh RF, Gadi VK, Guenthoer J, Beumer JH, Korde L, Strychor S, Kiesel BF, Linden HM, Thompson JA, Swisher E, Chai X, Shepherd S, Giranda V, Specht JM. Phase I Study of Veliparib (ABT-888) Combined with Cisplatin and Vinorelbine in Advanced Triple-Negative Breast Cancer and/or BRCA Mutation-Associated Breast Cancer. Clin Cancer Res. 2016 Jun 15;22(12):2855-64. doi: 10.1158/1078-0432.CCR-15-2137. PubMed PMID: 26801247; PubMed Central PMCID: PMC4911292.

15: Landrum LM, Brady WE, Armstrong DK, Moore KN, DiSilvestro PA, O'Malley DM, Tenney ME, Rose PG, Fracasso PM. A phase I trial of pegylated liposomal doxorubicin (PLD), carboplatin, bevacizumab and veliparib in recurrent, platinum-sensitive ovarian, primary peritoneal, and fallopian tube cancer: An NRG Oncology/Gynecologic Oncology Group study. Gynecol Oncol. 2016 Feb;140(2):204-9. doi: 10.1016/j.ygyno.2015.11.024. PubMed PMID: 26616225; PubMed Central PMCID: PMC4724478.

16: Gupta SK, Kizilbash SH, Carlson BL, Mladek AC, Boakye-Agyeman F, Bakken KK, Pokorny JL, Schroeder MA, Decker PA, Cen L, Eckel-Passow JE, Sarkar G, Ballman KV, Reid JM, Jenkins RB, Verhaak RG, Sulman EP, Kitange GJ, Sarkaria JN. Delineation of MGMT Hypermethylation as a Biomarker for Veliparib-Mediated Temozolomide-Sensitizing Therapy of Glioblastoma. J Natl Cancer Inst. 2015 Nov 27;108(5). pii: djv369. doi: 10.1093/jnci/djv369. PubMed PMID: 26615020; PubMed Central PMCID: PMC4862419.

17: Gabrielson A, Tesfaye AA, Marshall JL, Pishvaian MJ, Smaglo B, Jha R, Dorsch-Vogel K, Wang H, He AR. Phase II study of temozolomide and veliparib combination therapy for sorafenib-refractory advanced hepatocellular carcinoma. Cancer Chemother Pharmacol. 2015 Nov;76(5):1073-9. doi: 10.1007/s00280-015-2852-2. PubMed PMID: 26449224; PubMed Central PMCID: PMC4612326.

18: Mizugaki H, Yamamoto N, Nokihara H, Fujiwara Y, Horinouchi H, Kanda S, Kitazono S, Yagishita S, Xiong H, Qian J, Hashiba H, Shepherd SP, Giranda V, Tamura T. A phase 1 study evaluating the pharmacokinetics and preliminary efficacy of veliparib (ABT-888) in combination with carboplatin/paclitaxel in Japanese subjects with non-small cell lung cancer (NSCLC). Cancer Chemother Pharmacol. 2015 Nov;76(5):1063-72. doi: 10.1007/s00280-015-2876-7. PubMed PMID: 26433581; PubMed Central PMCID: PMC4612330.

19: VanderWeele DJ, Paner GP, Fleming GF, Szmulewitz RZ. Sustained Complete Response to Cytotoxic Therapy and the PARP Inhibitor Veliparib in Metastatic Castration-Resistant Prostate Cancer - A Case Report. Front Oncol. 2015 Jul 22;5:169. doi: 10.3389/fonc.2015.00169. PubMed PMID: 26258074; PubMed Central PMCID: PMC4510409.

NMR, HPLC 99%, LCMS, Phthalimidoacetaldehyde, CAS: 2913-97-5, 1KG in stock, Pls check:

NMR, HPLC 99%, LCMS, COA, Pls check:

Product Name Phthalimidoacetaldehyde
Purity/Analysis Method >98.0%(N)
M.F. / M.W. C10H7NO3 / 189.17

CAS Number 2913-97-5

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

QQ: 2393923585

NMR, HPLC 99%, LCMS, Bis(pinacolato)diboron, CAS: 73183-34-3, 200KG in stock, Pls check:

NMR, HPLC 99%, LCMS, Bis(pinacolato)diboron, CAS: 73183-34-3, 200KG in stock, Pls check:

Bis(pinacolato)diboron
CAS Number：73183-34-3

CAS:73183-34-3
MF:C12H24B2O4
MW:253.94
EINECS:-0
Synonyms:BIS(2,2,3,3-TETRAMETHYL

Melting point:

137-140 °C(lit.)

storage temp. 

0-6°C

form 

Powder or Platelets

color 

White

Water Solubility 

Soluble in tetrahydrofuran, dichloromethane, toluene, hexane and heptane. Insoluble in water.

Merck 

1300

BRN 

7703552

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

NMR, HPLC 99%, LCMS, CAS: 1174020-45-1, 1KG in stock, Pls check:

NMR, HPLC, LCMA, COA, Pls kindly check:

Name: (3S,4S)-tert-Butyl 4-fluoro-3-hydroxypiperidine-1-carboxylate

CAS number 1174020-45-1

Formula C10H18FNO3

 

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

NMR, HPLC 99%, LCMS- AZD-3965, CAS: 1448671-31-5, 5g in stock

NMR,HPLC, LCMS, COA, Pls check:

Description: AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. In vivo, AZD3965 is well tolerated and induces a dose and time dependent accumulation of lactate in the tumours, suppresses tumour growth and in the Raji model potentiates the effects of Rituxan, doxorubicin and bendamustine. The selective inhibition of lactate transport by the MCT1 inhibitor AZD3965 offers an novel mechanism for targeting the metabolic phenotype in tumours that preferentially express MCT1.

Name: AZD-3965 

CAS#: 1448671-31-5 (or 733809-45-5) 

Chemical Formula: C21H24F3N5O5S 

Exact Mass: 515.14502 

Molecular Weight: 515.50597 

Elemental Analysis: C, 48.93; H, 4.69; F, 11.06; N, 13.59; O, 15.52; S, 6.22

Synonym: AZD3965; AZD-3965; AZD 3965.

IUPAC/Chemical Name: (S)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((3-methyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione

InChi Key: PRNXOFBDXNTIFG-FQEVSTJZSA-N

InChi Code: InChI=1S/C21H24F3N5O5S/c1-9(2)29-18-14(16(30)27(5)19(29)32)13(17(31)28-7-20(4,33)8-34-28)12(35-18)6-11-10(3)25-26-15(11)21(22,23)24/h9,33H,6-8H2,1-5H3,(H,25,26)/t20-/m0/s1

SMILES Code: O=C1N(C(C)C)C2=C(C(C(N3OC[C@@](C)(O)C3)=O)=C(CC4=C(C(F)(F)F)NN=C4C)S2)C(N1C)=O

TECHNICAL DATA

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

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).

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

ADDITIONAL INFORMATION

AZD3965 sensitivity varied in vitro and was highest in hypoxia. Resistance in hypoxia was associated with increased MCT4 expression. In vivo, AZD3965 reduced tumor growth and increased intra-tumor lactate. In the tissue microarray, high MCT1 expression was associated with worse prognosis (p=0.014). MCT1 and hypoxia marker CA IX expression in the absence of MCT4 was observed in 21% of SCLC tumor   

 REFERENCES

1: Blackhall F. O11.5Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Ann Oncol. 2015 Mar;26 Suppl 2:ii15. doi: 10.1093/annonc/mdv089.5. PubMed PMID: 25795820.

2: Lamb R, Harrison H, Hulit J, Smith DL, Lisanti MP, Sotgia F. Mitochondria as new therapeutic targets for eradicating cancer stem cells: Quantitative proteomics and functional validation via MCT1/2 inhibition. Oncotarget. 2014 Nov 30;5(22):11029-37. PubMed PMID: 25415228; PubMed Central PMCID: PMC4294326.

3: Marchiq I, Le Floch R, Roux D, Simon MP, Pouyssegur J. Genetic disruption of lactate/H+ symporters (MCTs) and their subunit CD147/BASIGIN sensitizes glycolytic tumor cells to phenformin. Cancer Res. 2015 Jan 1;75(1):171-80. doi: 10.1158/0008-5472.CAN-14-2260. Epub 2014 Nov 17. PubMed PMID: 25403912.

4: Bola BM, Chadwick AL, Michopoulos F, Blount KG, Telfer BA, Williams KJ, Smith PD, Critchlow SE, Stratford IJ. Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport. Mol Cancer Ther. 2014 Dec;13(12):2805-16. doi: 10.1158/1535-7163.MCT-13-1091. Epub 2014 Oct 3. PubMed PMID: 25281618; PubMed Central PMCID: PMC4258406.

5: Polański R, Hodgkinson CL, Fusi A, Nonaka D, Priest L, Kelly P, Trapani F, Bishop PW, White A, Critchlow SE, Smith PD, Blackhall F, Dive C, Morrow CJ. Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Clin Cancer Res. 2014 Feb 15;20(4):926-37. doi: 10.1158/1078-0432.CCR-13-2270. Epub 2013 Nov 25. PubMed PMID: 24277449; PubMed Central PMCID: PMC3929348.

NMR, HPLC 99%, LCMS- Acalabrutinib (ACP-196), CAS: 748788-37-6, 1kg in stock

NMR HPLC, LCMS, COA, pls kindly check:

Acalabrutinib (ACP-196)
Description: Acalabrutinib, also known as ACP-196, is an orally available inhibitor of Bruton’s tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

Name: Acalabrutinib (ACP-196) 
CAS#: 1420477-60-6 
Chemical Formula: C26H23N7O2 
Exact Mass: 465.19132 
Molecular Weight: 465.52 
Elemental Analysis: C, 67.08; H, 4.98; N, 21.06; O, 6.87

Synonym: ACP-196; ACP196; ACP 196; Acalabrutinib
IUPAC/Chemical Name: (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide
InChi Key: WDENQIQQYWYTPO-IBGZPJMESA-N
InChi Code: InChI=1S/C26H23N7O2/c1-2-6-21(34)32-15-5-7-19(32)25-31-22(23-24(27)29-14-16-33(23)25)17-9-11-18(12-10-17)26(35)30-20-8-3-4-13-28-20/h3-4,8-14,16,19H,5,7,15H2,1H3,(H2,27,29)(H,28,30,35)/t19-/m0/s1
SMILES Code: O=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C([C@H]5N(C(C#CC)=O)CCC5)=N3)C=C2

TECHNICAL DATA
Appearance: Yellow solid powder
Purity: >98% (or refer to the Certificate of Analysis)

ADDITIONAL INFORMATION
Acalabrutinib is a potent and selective BTK (Bruton's tyrosine kinase) inhibitor. BTK is a cytoplasmic, non-receptor tyrosine kinase that transmits signals from a variety of cell-surface molecules, including the B-cell receptor (BCR) and tissue homing receptors. Genetic BTK deletion causes B-cell immunodeficiency in humans and mice, making this kinase an attractive therapeutic target for B-cell disorders. BTK inhibitors targeting B cell receptor signaling and other survival mechanism showed great promise for the treatment of chronic lymphocytic leukemia (CLL)s holds great promise.
As of 2015 it is in late stage clinical trials for relapsed chronic lymphocytic leukemia. Interim results are encouraging : 95% overall response rate. It is also in another 20 clinical trials (alone and in combination) for various cancers.

2017 China CPHI: E1M35

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REFERENCES
1: Maly J, Blachly JS. Chronic Lymphocytic Leukemia: Exploiting Vulnerabilities with Targeted Agents. Curr Hematol Malig Rep. 2016 Feb 11. [Epub ahead of print] PubMed PMID: 26893063.
2: Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT, Brown JR, Hillmen P, Stephens DM, Ghia P, Barrientos JC, Pagel JM, Woyach J, Johnson D, Huang J, Wang X, Kaptein A, Lannutti BJ, Covey T, Fardis M, McGreivy J, Hamdy A, Rothbaum W, Izumi R, Diacovo TG, Johnson AJ, Furman RR. Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. N Engl J Med. 2016 Jan 28;374(4):323-32. doi: 10.1056/NEJMoa1509981. Epub 2015 Dec 7. PubMed PMID: 26641137.