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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-Pirtobrutinib
Pirtobrutinib

Chemical Structure : Pirtobrutinib

CAS No.: 2101700-15-4

Pirtobrutinib (LOXO-305, LOXO305, LY3527727, RXC-005)

货号: PC-72630Not For Human Use, Lab Use Only.

Pirtobrutinib (LOXO-305, LY3527727, RXC-005) is a highly potent and selective non-covalent BTK inhibitor with IC50 of 5.69 nM, shows nanomolar potency against both wild-type and C481-mutated BTK.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Pirtobrutinib (LOXO-305, LY3527727, RXC-005) is a highly potent and selective non-covalent BTK inhibitor with IC50 of 5.69 nM.
LOXO-305 shows nanomolar potency against both wild-type and C481-mutated BTK.
LOXO-305 displays >300 fold selectivity on BTK over 98% of other kinases, reducing the potential for off-target toxicities.
Pirtobrutinib (LOXO-305) has been designed to maintain greater than 90% of maximal BTK inhibition at trough, thereby achieving effective target inhibition throughout the dosing interval, even in proliferative tumours.

物理化学性质&存储条件

分子量 479.436
分子式 C22H21F4N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-amino-3-[4-[[(5-fluoro-2-methoxybenzoyl)amino]methyl]phenyl]-1-[(2S)-1,1,1-trifluoropropan-2-yl]pyrazole-4-carboxamide

参考文献

1. Brandhuber B, et al. Clin. Lymphoma Myeloma Leuk. 2018;18:S216.

2. Ito K, et al. Eur J Cancer. 2021 Mar;145:183-193.

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