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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Trk Receptor-LPM4870108
LPM4870108

Chemical Structure : LPM4870108

CAS No.: 2803679-07-2

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LPM4870108 (LPM-4870108)

货号: PC-25354Not For Human Use, Lab Use Only.

LPM4870108 is a next‐generation, potent pan-Trk inhibitor with IC50 of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively, shows high selectivity over ALK (IC50=182 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LPM4870108 is a next‐generation, potent pan-Trk inhibitor with IC50 of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively, shows high selectivity over ALK (IC50=182 nM).
LPM4870108 (5, 10, or 20 mg/kg) produced significant inhibition of tumor growth both in wild-type NTRK fusion mutation cells (Ba/F3 LMNA-NTRK1cells and Ba/F3 ETV6-NTRK3 cells) and drug-resistant mutation cells (Ba/F3 ETV6-NTRK3-G623R cells and Ba/F3 LMNA-NTRK1-G595R).
LPM4870108 is more efficacious and safer against tumor growth than LOXO-195.

物理化学性质&存储条件

分子量 410.41
分子式 C20H19FN6O3
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

(S,3'E,4'E)-5'-fluorospiro[cyclopropane-1,6'-4-oxa-7-aza-2(4,3)-morpholina-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridinacyclooctaphan]-8'-one

参考文献

1. Liu B, et al. J Clin Invest. 2025 Aug 12:e194879.

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