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PCI-32765 Racemate

Catalog No.GC12921

PCI-32765 Racemate(PCI-32765 Racemate)는 Ibrutinib의 라세미체입니다. 이브루티닙은 IC50 값이 0.5nM인 선택적 비가역적 Btk 억제제입니다.

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PCI-32765 Racemate Chemical Structure

Cas No.: 936563-87-0

Size 가격 재고 수량
5mg
US$41.00
재고 있음
10mg
US$57.00
재고 있음
50mg
US$165.00
재고 있음
200mg
US$324.00
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

PCI-32765 is an inhibitor of Bruton tyrosine kinase (BTK) with IC50 value of 0.5nM [1].

PCI-32765 is a covalent and irreversible inhibitor of BTK through bonding to Cys-481 in the ATP binding domain. PCI-32765 inhibits phosphorylation of BTK in a B cells (IC50 of 11nM) as well as the downstream substrates phosphoinositide phospholipase Cγ (PLC γ) and ERK in cell assays. PCI-32765 has in vivo efficacy in B cell lymphoma. In CLL cells, PCI-32765 induces cells apoptosis through inhibiting the expression of BCR-dependent UDP-glucose ceramide glucosyltransferase [1].

PCI-32765 is oral effective in vivo. It induces lymphocytosis during the first weeks of therapy in patients with CLL. It is also efficacious in autoimmune disease. In the MRL-Fas lupus model, PCI-32765 inhibits collagen-induced arthritis as well as autoantibody production and development of kidney disease. It also diminished FcγRIII-induced production of pro-inflammatory cytokines [1].

References:
[1] Burger JA, Buggy JJ. Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765). Leuk Lymphoma. 2013 Nov;54(11):2385-91.

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