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2018年3月8日星期四

Top acalabrutinib (ACP-196; 1420477-60-6) GMP Manufacture and acalabrutinib intermediates

GMP, ISO custom synthesis Medicinal Chemistry; FDA new API and Intermediates, HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided.

Teva, Novartis, Pfizer, Hikma, Glenmark, Gilead all Site Audit approved us.

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1.

Acalabrutinib , ACP-196, CAS# 1420477-60-6, HPLC 99.62%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 100g in stock

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

 

2.

Acalabrutinib Intermediates:


Acalabrutinib Intermediates,  CAS# 1420478-88-1(S)-benzyl 2-(8-amino-1-bromoimidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylateHPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.

Acalabrutinib Intermediates,  CAS# 1383385-64-5 N-Pyridin-2-yl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl) -benzamideHPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.

Acalabrutinib Intermediates,  CAS# 1420478-89-2HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.

Acalabrutinib Intermediates,  CAS#1420478-90-5HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.


Acalabrutinib Intermediates,  CAS#1418307-18-2HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.


Acalabrutinib Intermediates,  CAS#1418307-17-1HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.

Acalabrutinib Intermediates,  CAS#864759-39-7HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.

Acalabrutinib Intermediates,  CAS#850568-25-14-(Pyridin-2-yl)aminocarbonylphenylboronicacid, HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.


Acalabrutinib Intermediates,  CAS#939412-86-9, (3-Chloropyrazin-2-yl)MethanaMine hydrochloride, HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided, More than 100g in stock.


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.

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.

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