1. Protein Tyrosine Kinase/RTK
  2. ALK
  3. TPX-0131

TPX-0131 

Cat. No.: HY-139279
Handling Instructions

TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities.

For research use only. We do not sell to patients.

TPX-0131 Chemical Structure

TPX-0131 Chemical Structure

CAS No. : 2648641-36-3

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Description

TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities[1].

IC50 & Target

IC50: 1.4 nM (Wild-typr AKT); 0.2-6.6 nM (mutant ALK variants)[1]

In Vitro

TPX-0131 potently inhibits wild-type ALK (IC50 = 1.4 nM) and 26 ALK resistance mutations. 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 IC50 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 IC50 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TPX-0131 (2-10 mg/kg; p.o.; twice a day; for 2 weeks) treatment at 2 mg/kg, 5 mg/kg, and 10 mg/kg resulted in dose-dependent tumor growth inhibition (TGI) of 64%, 120%, and 200% (complete regression), respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female SCID/beige mice (5-8 weeks old) bearing Ba/F3 cells[1]
Dosage: 2 mg/kg, 5 mg/kg, and 10 mg/kg
Administration: p.o.; twice a day; for 2 weeks
Result: Caused complete tumor regression in ALK mutation-dependent xenograft models.
Molecular Weight

447.41

Formula

C₂₁H₂₀F₃N₅O₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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TPX-0131
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