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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-OBX02-011
OBX02-011

Chemical Structure : OBX02-011

CAS No.: 2349336-18-9

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OBX02-011 (OBX 02-011)

货号: PC-47006Not For Human Use, Lab Use Only.

OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.

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5 mg ￥2480 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg Get quote
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

OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.
OBX02-011 occupied the ATP-binding site in a similar manner to WZ-4002.
OBX02-011 showed broad activity at low nanomolar concentrations against mutant EGFRs, more potent in Del19/T790M/C797S and L858R/T790M than in other EGFR mutations.
OBX02-011 was highly effective against EGFR triple mutations, and showed substantial selectivity compared with WT EGFR (IC50= 1471 nM in WT, 96.3 nM in Del19/T790M/C797S, and 94.8 nM in L858R/T790M/C797S) in Ba/F3 cell lines expressing EGFR.
OBX02-011 (25 mg/kg, i. p.) effectively inhibited tumor growth and EGFR activity, leading to enhanced survival in transgenic mouse models (EGFRL858R/T790M/C797S).

物理化学性质&存储条件

分子量 615.194
分子式 C29H39ClN8O3S
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-((5-chloro-2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)-N-methylmethanesulfonamide

参考文献

1. Yun Jung Choi, et al. Cancer Res. 2022 Jun 14;canres.0394.2022-2-3 21:03:12.200.

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