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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MAP4K-BGB-15025
BGB-15025

Chemical Structure : BGB-15025

CAS No.: 2766481-17-6

BGB-15025 (BGB15025)

货号: PC-23066Not For Human Use, Lab Use Only.

BGB-15025 is a potent and selective hematopoietic progenitor kinase 1 (HPK1) inhibitor with biochemical IC50 of 1.04 nM.

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

生物&药学活性

BGB-15025 is a potent and selective hematopoietic progenitor kinase 1 (HPK1) inhibitor with biochemical IC50 of 1.04 nM.
BGB-15025 shows good selectivity profile among MAP4K family and does not affect ZAP70 phosphorylation up to 1 μM.
BGB-15025 potently reduces SLP76 phosphorylation and increase downstream ERK phosphorylation in a concentration dependent manner in T cells-based assay.
BGB-15025 induces TCR activation and IL-2 production in T cells.
Oral administration of BGB-15025 demonstrates dose-dependent pSLP76 inhibition in splenic T cells and induces serum IL-2 in mouse model.
BGB-15025 exhibits anti-tumor activity in GL261 tumor model as single agent, also demonstrated combination effect with anti-PD-1 antibody in CT26 and EMT-6 syngeneic tumor models.

物理化学性质&存储条件

分子量 536.66
分子式 C28H37FN8O2
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

Benzamide, 4-[5-amino-6-[[1-(1-methyl-4-piperidinyl)-1H-pyrazol-4-yl]oxy]-2-pyrazinyl]-N-[2-[(3R)-3-fluoro-1-pyrrolidinyl]ethyl]-2,6-dimethyl-

参考文献

1. Ye Liu, et al. Cancer Res (2022) 82 (12_Supplement): 5541.

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