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首页-小分子抑制剂&激动剂-Tyrosine Kinase-ROS1-Lorlatinib
Lorlatinib

Chemical Structure : Lorlatinib

CAS No.: 1454846-35-5

Lorlatinib (PF-06463922, PF 06463922, PF06463922)

货号: PC-42919Not For Human Use, Lab Use Only.

Lorlatinib (PF-06463922) is a potent, CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with IC50 of 0.07/0.025 nM respectively.

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

生物&药学活性

Lorlatinib (PF-06463922) is a potent, CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with IC50 of 0.07/0.025 nM respectively.
Lorlatinib (PF-06463922) also inhibits ALK L1196M (IC50=0.7 nM) and exhibits selectivity >100-fold for ROS1 over 204 kinases.
Lorlatinib (PF-06463922) inhibits crizotinib-resistant mutant ROS1G2032R and ROS1L2026M and orally available in vivo.

物理化学性质&存储条件

分子量 406.413
分子式 C21H19FN6O2
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

DMSO: ≥ 28 mg/mL

Chemical Name/SMILES

2H-4,8-Methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile, 7-amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-, (10R)-

参考文献

1. Zou HY, et al. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8.

2. Johnson TW, et al. J Med Chem. 2014 Jun 12;57(11):4720-44.

3. Infarinato NR, et al. Cancer Discov. 2016 Jan;6(1):96-107.

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