Zotizalkib (TPX-0131) | ALK inhibitor | Probechem Biochemicals

Chemical Structure : TPX-0131

CAS No.: 2648641-36-3

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TPX-0131 (Zotizalkib, TPX0131)

货号: PC-72509Not For Human Use, Lab Use Only.

TPX-0131 (Zotizalkib, TPX0131) is a potent, CNS-penetrant, next-generation inhibitor of wild-type ALK (IC50=1.4 nM) and 26 ALK resistance mutations (all IC50=<1-7 nM).

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5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5880	In stock
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生物&药学活性

TPX-0131 (Zotizalkib, TPX0131) is a potent, CNS-penetrant, next-generation inhibitor of wild-type ALK (IC50=1.4 nM) and 26 ALK resistance mutations (all IC50=<1-7 nM).
TPX-0131 is highly potent against a broad spectrum of ALK drug-resistant mutations. TPX-0131 inhibited C1156Y, E1210K/S1206C, L1198F/C1156Y, L1196M/L1198F, E1210K, L1196M, T1151M, deleted G1202, S1206R, G1202R/L1198F, F1174L, F1245C, R1275Q, and G1202R ALK mutations with IC50 values of <1 nM.
TPX-0131 had IC50 values of 1 to 2 nM for the following ALK mutations: L1198F, L1152R, F1174S, T1151-L1152 insT, V1180L, G1269A, F1174C.
TPX-0131 was less active against ALK mutations including I1171N, L1152P, D1203N, D1203N/E1210K, and G1269S, with IC50 values of 2-7 nM.
TPX-0131 was determined to be a selective ALK inhibitor by evaluating its potency toward a panel of 373 kinases.
TPX-0131 potently inhibits WT EML4-ALK and EML4-ALK harboring a range of point mutations with significantly greater potency against many key resistance mutations, such as solvent front, gatekeeper, and hinge region mutations, relative to previous generations of ALK inhibitors.
TPX-0131 exhibited more than 90% phosphorylation inhibition of EML4-ALK G1202R/L1196M fusion at a mean free plasma concentration of 19.5 nM, demonstrated tumor growth in the EML4-ALK G1202R/L1196M xenograft model.

物理化学性质&存储条件

分子量	447.418
分子式	C21H20F3N5O3
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	(4S)-4-(difluoromethyl)-8-fluoro-13,13-dimethyl-3,4,13,14-tetrahydro-6H-18,1-(metheno)[1,4]oxazino[3,4-i]pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-15(12H)-one

参考文献

1. Brion W Murray, et al. Mol Cancer Ther. 2021 Sep;20(9):1499-1507.

TPX-0131 (Zotizalkib, TPX0131)

生物&药学活性

物理化学性质&存储条件

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TPX-0131 (Zotizalkib, TPX0131)

生物&药学活性

物理化学性质&存储条件

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