TPX-0131
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $1750 | Check With Us |
500mg | $2600 | Check With Us |
1g | $3900 | Check With Us |
Cat #: V2490 CAS #: 2648641-36-3 Purity ≥ 99%
Description: TPX 0131 (TPX-0131) is a novel, potent CNS-penetrant ALK inhibitor with anticancer activity.
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Molecular Weight (MW) | 447.41 |
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Molecular Formula | C21H20F3N5O3 |
CAS No. | 2648641-36-3 |
SMILES Code | FC([C@H]1N2C3=NC4=C(C(NC(C)(COC5=CC=C(F)C=C5C2)C)=O)C=NN4C=C3OC1)F |
Synonyms | TPX-0131; TPX 0131; TPX0131; Zotizalkib |
Protocol | In Vitro | Zotizalkib 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. Zotizalkib potently inhibits wild-type ALK (IC50=1.4 nM) and 26 ALK resistance mutations. Zotizalkib 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. Zotizalkib has IC50 values of 1-2 nM for the following ALK mutations: L1198F, L1152R, F1174S, T1151-L1152 insT, V1180L, G1269A, F1174C. Zotizalkib is less active against ALK mutations including I1171N, L1152P, D1203N, D1203N/E1210K, and G1269S, with IC50 values of 2-7 nM. |
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In Vivo | Zotizalkib (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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.2351 mL | 11.1754 mL | 22.3509 mL | 44.7017 mL |
5mM | 0.4470 mL | 2.2351 mL | 4.4702 mL | 8.9403 mL |
10mM | 0.2235 mL | 1.1175 mL | 2.2351 mL | 4.4702 mL |
20mM | 0.1118 mL | 0.5588 mL | 1.1175 mL | 2.2351 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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