PCI-32765 Racemate

PCI-32765 Racemate (PCI-32765 Racemate) 是依鲁替尼的外消旋体。 Ibrutinib 是一种选择性的、不可逆的 Btk 抑制剂，IC50 值为 0.5 nM。

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥512.00

410.00

- +
10mg

￥687.00

550.00

- +
50mg

￥2025.00

1620.00

- +
200mg

￥3950.00

3160.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci10084
CAS: 936563-87-0
别名: 1-[3-[4-氨基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶-1-基]哌啶-1-基]丙-2-烯-1-酮,PCI-32765 Racemate
分子式: C25H24N6O2
分子量: 440.5
纯度: >98%
溶解度: Soluble in DMSO
储存: 4°C, protect from light
库存: 现货

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].

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