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首页-小分子抑制剂&激动剂-Tyrosine Kinase-ROS1-JYP0322
JYP0322

Chemical Structure : JYP0322

CAS No.: 2644645-39-4

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JYP0322 (JYP-0322)

货号: PC-26641Not For Human Use, Lab Use Only.

JYP0322 is a potent, selective, next-generation, brain-penetrant macrocyclic ROS1 inhibitor with IC50 of 0.37 nM and 0.3 nM for ROS1 wild-type (WT) and ROS1G2032R, overcoming ROS1G2032R resistance.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JYP0322 is a potent, selective, next-generation, brain-penetrant macrocyclic ROS1 inhibitor with IC50 of 0.37 nM and 0.3 nM for ROS1 wild-type (WT) and ROS1G2032R, overcoming ROS1G2032R resistance.
JYP0322 demonstrates >130-fold selectivity over TRKA, shows moderate inhibition of TRKC (6-fold selectivity relative to ROS1) and weak activity against TRKB.
JYP0322 shows reduced potency against Ba/F3 LMNA-NTRK1 cells (IC50 = 37 nM) compared to repotrectinib (IC50 = 1.1 nM).
JYP0322 potently inhibits the proliferation of engineered cells with stable expression of CD74-ROS1 wild-type (WT) or clinically relevant mutants, including G2032R, S1986F/Y, G2033N, and G2101A.
JYP0322 demonstrated dose-dependent tumor growth inhibition (TGI) att doses of 1.5, 5, and 15 mg/kg administered twice daily (BID), achieved TGI rates of 83.5%, 101.4%, and 103.4%, respectively in Ba/F3 CD74-ROS1WT xenograft model.

物理化学性质&存储条件

分子量 421.39
分子式 C20H16FN7O3
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

(R,3'E,4'E)-5'-fluoro-8'-oxospiro[cyclopropane-1,6'-4-oxa-7-aza-2(2,3)-isoxazolidina-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridinacyclooctaphane]-2'-carbonitrile

参考文献

1. Yuxiang Ma, et al. Cancer Cell. 2026 Apr 23:S1535-6108(26)00172-8.

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