ICP-723 | pan-TRK inhibitor | Probechem Biochemicals

Chemical Structure : ICP-723

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ICP-723 (Zurletrectinib, ICP723)

货号: PC-22603Not For Human Use, Lab Use Only.

ICP-723 (Zurletrectinib) is a potent pan-TRK Inhibitor with IC50 of <1 nM for TRKA, TRKB and TRKC, potently inhibits activities of wild-type and some mutant forms of TRK.

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生物&药学活性

ICP-723 (Zurletrectinib) is a potent pan-TRK Inhibitor with IC50 of <1 nM for TRKA, TRKB and TRKC, potently inhibits activities of wild-type and some mutant forms of TRK.
ICP-723 (Zurletrectinib) competitively binds to TRKA/B/C with 100% of inhibition rate at 100 nM.
ICP-723 (Zurletrectinib) demonstrates robust in vitro efficacy in TRK-driven tumor cells, KM12 colorectal cancer cell line bearing TPM3-NTRK1 fusion, as well as a panel of 19 Ba/F3 pro-B murine cell lines over-expressing wild-type.
ICP-723 (Zurletrectinib) also overcomes solvent front mutations (e.g., TRKA G595R, TRKC G623R/E) often developed following 1st generation TRK inhibitor treatment.
ICP-723 (Zurletrectinib) exerts reduced activity in gatekeeper mutations (e.g., TRKA F589L, TRKB F633L, TRKC F617L) and some xDFG mutations (e.g., TRKA G667C/S, TRKB G709C); but retains activity in other xDFG mutations (e.g., TRKA G667A, TRKC G696A/C) and unclassified mutations (e.g., TRKA V573M, TRKA A608D, TRKB V689M).
ICP-723 (Zurletrectinib) (1 mg/kg) causes 89.5% TGI of KM12 tumors in xenograft models.
ICP-723 (Zurletrectinib) (1 or 3 mg/kg) leads to 100% survival of mice bearing Ba/F3 LMNA-NTRK1 G595R tumors, confirms the effectiveness of ICP-723 against solvent front mutant TRKA.

物理化学性质&存储条件

分子量	415.40
分子式	C19H19F2N7O2
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	10H-5,7-Ethenopyrazolo[4,3-g]pyrido[3,2-m]pyrrolo[1,2-k][1,4,6,9,11]oxatetraazacyclotetradecin-11(12H)-one, 2,18-difluoro-1,2,3,13,14,19b-hexahydro-14-methyl-, (2S,14S,19bR)-

参考文献

1. Ruixia Liang, et al. Cancer Res (2022) 82 (12_Supplement): 6187.

ICP-723 (Zurletrectinib, ICP723)

生物&药学活性

物理化学性质&存储条件

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ICP-723 (Zurletrectinib, ICP723)

生物&药学活性

物理化学性质&存储条件

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