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
EOS Med Chem produce Acalabrutinib (ACP-196) in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
First supplier who could produce EE, Optical purity 99.5 more, stock more than 20KG.
Acalabrutinib (ACP-196) Intermediates, EOS Med Chem have 8; Acalabrutinib (ACP-196) Impurity we have 10, all from GMP, FDA plant.
Now Acalabrutinib (ACP-196) DMF document is preparing.
Until 2016, Aug, Acalabrutinib (ACP-196) more than produced 25kg API, 120kg Intermediates, world biggest supplier.
Acalabrutinib (ACP-196) Intermediate 1420478-90-5,(S)-4-(8-amino-3-(pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide, HPLC99%, NMR, LCMS is ok, more than 100g in stock.
Acalabrutinib (ACP-196) Intermediate 1420478-89-2,(S)-benzyl 2-(8-amino-1-(4-(pyridin-2-ylcarbamoyl)phenyl)imidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylate,
Acalabrutinib (ACP-196) Intermediate 1420478-88-1, (S)-benzyl 2-(8-amino-1-bromoimidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylate,
Acalabrutinib (ACP-196) Intermediate 1420478-87-0,(S)-benzyl 2-(1-bromo-8-chloroimidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylate,
Acalabrutinib (ACP-196) Intermediate 1418307-18-2, (S)-benzyl 2-(8-chloroimidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylate, HPLC99%, NMR, LCMS is ok, more than 100g in stock.
Acalabrutinib (ACP-196) Intermediate 1418307-17-1, (S)-benzyl 2-((3-chloropyrazin-2-yl)methylcarbamoyl)pyrrolidine-1-carboxylate,
Acalabrutinib (ACP-196) Intermediate 771581-15-8, 2-Aminomethyl-3-chloropyrazine,
Acalabrutinib (ACP-196) Intermediate 55557-52-3, 3-Chloropyrazine-2-carbonitrile,
Acalabrutinib (ACP-196) Intermediate 1383385-64-5, No Name,
Acalabrutinib (ACP-196) Intermediate 180516-87-4, 4-Carboxylphenylboronic acid pinacol ester,
2017 China CPHI: E1M35
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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.
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
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.
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.
