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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-BLU-945
BLU-945

Chemical Structure : BLU-945

CAS No.: 2660250-10-0

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BLU-945 (ZL-2313, BLU945, BLU 945)

货号: PC-72903Not For Human Use, Lab Use Only.

BLU-945 (ZL-2313, BLU945, BLU 945) is a potent, mutant-selective inhibitor of EGFR T790M/C797S and EGFR+/T790M mutations (IC50<1 nM).

规格 价格 库存 数量
5 mg ￥1580 In stock
10 mg ￥2380 In stock
25 mg ￥3980 In stock
50 mg ￥5880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BLU-945 (ZL-2313, BLU945, BLU 945) is a potent, mutant-selective inhibitor of EGFR T790M/C797S and EGFR+/T790M mutations (IC50<1 nM).
BLU-945 inhibits EGFRex19del/T790M/C797S, EGFRL858R/T790M/C797S, EGFRex19del/T790M, and EGFRL858R/T790M mutants with sub-nanomolar IC50 values in an enzyme assay, with >1000-fold selectivity over EGFR WT.
BLU-945 achieves potent EGFR pathway inhibition in NCI-H1975 EGFRL858R/T790M, Ba/F3 EGFRL858R/T790M/C797S, and Ba/F3 EGFRex19del/T790M/C797S cell lines and a large window relative to EGFRWT inhibition.
Oral administration of BLU-945 to tumor-bearing mice demonstrated potent EGFR pathway inhibition and anti-tumor activity at well-tolerated doses in the subcutaneous NCI-H1975 CDX model, and osimertinib-resistant CDX and PDX models.

物理化学性质&存储条件

分子量 556.701
分子式 C28H37FN6O3S
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

N-(2-((3S,4R)-3-fluoro-4-methoxypiperidin-1-yl)pyrimidin-4-yl)-5-isopropyl-8-((2R,3S)-2-methyl-3-((methylsulfonyl)methyl)azetidin-1-yl)isoquinolin-3-amine

参考文献

1. Sun Min Lim, et al. Cancer Res (2021) 81 (13_Supplement): 1467.

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