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Chemical Structure : TPX-0131
CAS No.: 2648641-36-3
Catalog No.: 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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $588 | In stock | |
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| 100 mg | Get quote |
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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.
| M.Wt | 447.418 | |
| Formula | C21H20F3N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Brion W Murray, et al. Mol Cancer Ther. 2021 Sep;20(9):1499-1507.
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