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2016年3月14日星期一

So low price of Acalabrutinib (ACP-196), Why? / EOS Med Chem, Medicinal Chemical is Big

EOS Med Chem, now have 2 GMP plant in Taizhou city and ChongQing City. Regular produce some API and Intermediates and custom synthesis.

The plant have approved by CGMP, FDA, ISO. Customers TEVA, HIKMA, CIPLA, GLENMARK, MAYLAN and some others all audited.

Now my plant have 80 workers, 15 Tech person, 4 high Tech person.

And my source team have 4 source man, each one have more than 10 years in China market, they are clear COST and DELIVERY time.

Each day, we have new chemicals or price from my lab or plant.


Acalabrutinib (ACP-196)  1420477-60-6

As the world first commercial production, biggest suppliers.

Now we have 1000g in stock HPLC, NMR, MS we could provide.

Assay more than 98%+.

And we have 10 Intermediates could supply.

Welcome to ask me any interesting.

COA, HPLC, NMR as attachment







Below Acalabrutinib (ACP-196) Intermeidtes List, Assay more than 98%


1420478-90-5,(S)-4-(8-amino-3-(pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide
1420478-89-2,(S)-benzyl 2-(8-amino-1-(4-(pyridin-2-ylcarbamoyl)phenyl)imidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylate
1420478-88-1, (S)-benzyl 2-(8-amino-1-bromoimidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylate
1420478-87-0,(S)-benzyl 2-(1-bromo-8-chloroimidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylate
1418307-18-2, (S)-benzyl 2-(8-chloroimidazo[1,5-a]pyrazin-3-yl)pyrrolidine-1-carboxylate 
1418307-17-1, (S)-benzyl 2-((3-chloropyrazin-2-yl)methylcarbamoyl)pyrrolidine-1-carboxylate
771581-15-8,  2-Aminomethyl-3-chloropyrazine
55557-52-3, 3-Chloropyrazine-2-carbonitrile

1383385-64-5, No Name


180516-87-4, 4-Carboxylphenylboronic acid pinacol ester



2016 Shanghai CPHI, W5C47, Welcome!

EOS Med ChemMedchem is Big

執大象,天下往,往而無害,安平泰
網址www.eosmedchem.com 
辦公室: 0086-531-69905422-806(直通)
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Skype: willgutian

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 (last updated: 3/3/2016).
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
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

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.