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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 | $54 | In Stock | |
| 5 mg | $129 | In Stock | |
| 10 mg | $198 | In Stock | |
| 25 mg | $425 | In Stock | |
| 50 mg | $678 | In Stock | |
| 100 mg | $987 | In Stock | |
| 200 mg | $1,330 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $178 | 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 | TrkC:<1 nM, GOPC-ROS1:<1 nM, TPM3-TRKA:<1 nM, ALK:<4 nM, ALK (variants):<4 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]. |
| Synonyms | 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/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 33 mg/mL (52.02 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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