This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
TPX-0131
Catalog No. T9414 CAS
2648641-36-3
TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK ( IC 50 of 1.4 nM) and is potent against ALK-resistant mutation, e.g. G1202R ( IC 50 of 0.3 nM), L1196M ( IC 50 of 0.3 nM). TPX-0131 has strong antitumor activities [1].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK ( IC 50 of 1.4 nM) and is potent against ALK-resistant mutation, e.g. G1202R ( IC 50 of 0.3 nM), L1196M ( IC 50 of 0.3 nM). TPX-0131 has strong antitumor activities [1].
In vitro
TPX-0131 potently inhibits the resistance mutations of wild-type ALK (IC 50 = 1.4 nM) and 26 ALK. TPX-0131 inhibits 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. TPX0131 has IC 50 values of 1-2 nM for the following ALK mutations: L1198F, L1152R, F1174S, T1151-L1152 insT, V1180L, G1269A, F1174C. TPX-0131 is less active against ALK mutations including I1171N, L1152P, D1203N, D1203N/E1210K, and G1269S, with IC 50 values of 2-7 nM [1]. TPX-0131 is a potent inhibitor of ALK autophosphorylation in Ba/F3 cells expressing EML4-ALK G1202R solvent front, EML4-ALK G1202R/L1196M, or EML4-ALK G1202R/L1198F mutations, with IC50 values of approximately 3-10 nM [1].
In vivo
TPX-0131 administered orally at doses of 2 mg/kg, 5 mg/kg, and 10 mg/kg twice daily for two weeks to female SCID/beige mice (5-8 weeks old) bearing Ba/F3 cells demonstrated dose-dependent tumor growth inhibition (TGI) of 64%, 120%, and 200% (complete regression), respectively, in ALK mutation-dependent xenograft models [1].
Molecular Weight
447.41
Formula
C21H20F3N5O3
CAS No.
2648641-36-3
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.