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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-CK-101
CK-101

Chemical Structure : CK-101

CAS No.: 1660963-42-7

CK-101 (Olafertinib, RX-518)

货号: PC-61597Not For Human Use, Lab Use Only.

CK-101 (Olafertinib, RX-518) is a novel potent, mutant-selective, irreversible, orally available EGFR inhibitor, overcomes T790M-mediated resistance in NSCLC.

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25 mg ¥4280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CK-101 (Olafertinib, RX-518) is a novel potent, mutant-selective, irreversible, orally available EGFR inhibitor, overcomes T790M-mediated resistance in NSCLC.
CK-101 (Olafertinib, RX-518) specifically targets the mutant forms of EGFR, including T790M, while exhibiting minimal activity toward WT EGFR.
CK-101 (Olafertinib, RX-518) selectively inhibits cell proliferation of cell lines expressing both the activating (HCC827, IC50 <15 nM) and resistance mutations (NCI-H1975, IC50 <5 nM).
CK-101 (Olafertinib, RX-518) significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft models, with no activity in WT EGFR tumor xenograft model.

物理化学性质&存储条件

分子量 530.58
分子式 C29H28F2N6O2
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-[3-[2-[2,3-difluoro-4-[4-(2-hydroxyethyl)piperazin-1-yl]anilino]quinazolin-8-yl]phenyl]prop-2-enamide

参考文献

1. Xiangping Qian, et al. Abstract 2078: CK-101 (RX518), a mutant-selective inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. DOI: 10.1158/1538-7445.AM2017-2078

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