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Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $60 | In Stock | |
2 mg | $85 | In Stock | |
5 mg | $147 | In Stock | |
10 mg | $239 | In Stock | |
25 mg | $488 | In Stock | |
50 mg | $712 | In Stock | |
100 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $198 | In Stock |
Description | Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM. |
Targets&IC50 | ALK (variants):<4 nM, GOPC-ROS1:<1 nM, ALK:<4 nM, TrkC:<1 nM, TPM3-TRKA:<1 nM |
In vitro | Ensartinib potently inhibits both wild-type ALK and all evaluated ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM. Besides ALK, ensartinib also potently inhibits GOPC-ROS1, TPM3-TRKA, and TRKC with an IC50 of <1 nM, and inhibits EphA1, EphA2, EphB1 and c-MET with an IC50 of 1-10 nM[1]. |
Alias | X-396 dihydrochloride, Ensartinib dihydrochloride |
Molecular Weight | 634.36 |
Formula | C26H29Cl4FN6O3 |
Cas No. | 2137030-98-7 |
Smiles | Cl.Cl.C[C@@H](Oc1cc(nnc1N)C(=O)Nc1ccc(cc1)C(=O)N1C[C@H](C)N[C@H](C)C1)c1c(Cl)ccc(F)c1Cl |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 33 mg/mL (52.02 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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