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PCI-32765 Racemate

Catalog No.
B3242
BTK抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,572.00
Ship with 10-15 days
10mg
¥ 2,830.00
Ship with 10-15 days
50mg
¥ 8,579.00
Ship with 10-15 days
100mg
¥ 12,137.00
Ship with 10-15 days

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Background

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.

Chemical Properties

StorageStore at RT
M.Wt440.5
Cas No.936563-87-0
FormulaC25H24N6O2
SolubilitySoluble in DMSO
Chemical Name1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
SDFDownload SDF
Canonical SMILESC=CC(=O)N1CCCC(C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

PCI-32765 Racemate