| Identification | Back Directory | [Name]
X-376 | [CAS]
1365267-27-1 | [Synonyms]
X-376
X-396
CS-1720
Ensartinib
(R)-6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-N-(4-(4-methylpiperazine-1-carbonyl)phenyl)pyridazine-3-carboxamide
6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide
6-Amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-3-pyridazinecarboxamide
3-Pyridazinecarboxamide, 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]- | [Molecular Formula]
C25H25Cl2FN6O3 | [MDL Number]
MFCD25976868 | [MOL File]
1365267-27-1.mol | [Molecular Weight]
547.409 |
| Chemical Properties | Back Directory | [Boiling point ]
695.1±55.0 °C(Predicted) | [density ]
1.428±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Ethanol:13.0(Max Conc. mg/mL);23.75(Max Conc. mM) | [form ]
A crystalline solid | [pka]
10.70±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
X-376 is an ALK inhibitor with potential efficacy in the treatment of non-small cell lung cancer. | [Side effects]
The more common side effects of X-376 treatment include rash, itching, edema, and anemia. | [Physiological effects]
Ensatinib (X-376) is a second-generation tyrosine kinase inhibitor (TKI) small-molecule targeted drug targeting ALK fusion, which can selectively bind to the products of two driver gene mutations, ALK and MET. Block the activation and transmission of downstream signaling pathways, thereby inhibiting the growth and proliferation of cancer cells with these mutations, and exerting anti-cancer effects. | [in vivo]
The effects of X-376 in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that X-376 shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with X-376 at 50 mg/kg bid. X-376 significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, X-376 appears well-tolerated in vivo. Mouse weight is unaffected by X-376 treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of X-376, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of X-376 at 25, 50, 100 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 50 mg/kg for X-376. At NST levels, X-376 achieves an AUC of 41 μM×hr and a Cmax of 5.04 μM[1]. | [IC 50]
ALK: 0.61 nM (IC50) |
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