1. Protein Tyrosine Kinase/RTK
  2. ALK
    c-Met/HGFR

Ensartinib (Synonyms: X-396)

Cat. No.: HY-103714
Handling Instructions

X-396 is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.

For research use only. We do not sell to patients.

Ensartinib Chemical Structure

Ensartinib Chemical Structure

CAS No. : 1370651-20-9

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Description

X-396 is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.

IC50 & Target

IC50: <0.4 nM (ALK), 0.74 nM (MET)[1]

In Vitro

The ability of X-396 to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. X-396 is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). X-396 is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 9 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC50s of 68 nM, 156 nM, 9.644 μM and 2.989 μM, respectively[1].

In Vivo

The effects of X-396 in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that X-396 shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with X-396 at 25mg/kg bid. X-396 significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, X-396 appears well-tolerated in vivo. Mouse weight is unaffected by X-396 treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of X-396, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of X-396 at 20, 40, 80 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80mg/kg for X-396. At NST levels, X-396 achieves an AUC of 66 μM×hr and a Cmax of 7.19 μM[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7811 mL 8.9057 mL 17.8113 mL
5 mM 0.3562 mL 1.7811 mL 3.5623 mL
10 mM 0.1781 mL 0.8906 mL 1.7811 mL
*Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

For viability experiments, cells are seeded in 96-well plates at 25%-33% confluency and exposed to drugs.The human lung adenocarcinoma cell lines H3122 and H2228 are treated with X-396 (10, 30, 100, 300 and 1000 nM). SUDHL-1 lymphoma cells are treated with X-396 (5, 10, 30, 100 and 300 nM). SY5Y neuroblastoma cells are treated with X-396 (30, 100, 300 and 1000 nM). At 72 hours post X-396 addition, Cell Titer Blue Reagent is added and fluorescence is measured on a Spectramax spectrophotometer. All experimental points are set up in hextuplicate replicates and are performed at least two independent times. IC50s are calculated using GraphPad Prism version 5 for Windows. The curves are fit using a nonlinear regression model with a log (inhibitor) vs. response formula[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Nude mice (nu/nu) are injected with H3122 cells. Once tumors reach an average volume of 450 mm3, a total of 27 athymic mice harboring H3122 tumors are randomized and dosed via oral gavage with 25mg/kg X-396 or the control vehicle. Two, five, and fifteen hours after the single treatment (3 tumors/timepoint/group), mice are sacrificed and serum is collected for assessment of drug concentration using an LC-MS based bioanalytical method.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

561.44

Formula

C₂₆H₂₇Cl₂FN₆O₃

CAS No.

1370651-20-9

SMILES

O=C(C1=NN=C(N)C(O[[email protected]@H](C2=C(Cl)C=CC(F)=C2Cl)C)=C1)NC3=CC=C(C(N4C[[email protected]@H](C)N[[email protected]@H](C)C4)=O)C=C3

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

  • 不定价,药明ref丁佳丽要求上线20180706;竞价
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Ensartinib
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Ensartinib

Cat. No.: HY-103714