1. Protein Tyrosine Kinase/RTK
  2. Anaplastic lymphoma kinase (ALK)
  3. TPX-0131

TPX-0131 

Cat. No.: HY-139279 Purity: ≥95.0%
COA 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

Size Price Stock Quantity
5 mg USD 370 In-stock
Estimated Time of Arrival: December 31
10 mg USD 590 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1880 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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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.
Clinical Trial
Molecular Weight

447.41

Formula

C21H20F3N5O3

CAS No.
SMILES

FC([[email protected]]1N2C3=NC4=C(C(NC(C)(COC5=CC=C(F)C=C5C2)C)=O)C=NN4C=C3OC1)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (55.88 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2351 mL 11.1754 mL 22.3509 mL
5 mM 0.4470 mL 2.2351 mL 4.4702 mL
10 mM 0.2235 mL 1.1175 mL 2.2351 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: ≥95.0%

References
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Product Name:
TPX-0131
Cat. No.:
HY-139279
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