Ensartinib

Modify Date: 2026-06-30 19:35:32

Ensartinib structure	Common Name	Ensartinib
	CAS Number	1365267-27-1	Molecular Weight	547.409
	Density	1.4±0.1 g/cm3	Boiling Point	695.1±55.0 °C at 760 mmHg
	Molecular Formula	C₂₅H₂₅Cl₂FN₆O₃	Melting Point	N/A
	MSDS	N/A	Flash Point	374.2±31.5 °C

Use of Ensartinib

X-376 is a potent and dual ALK/MET inhibitor with IC50s of 0.61 nM and 0.69 nM, respectively.

This table lists Chinese names, IUPAC names and various aliases of this chemical substance.

Name	6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide
Synonym	More Synonyms

This table contains bioactivity, target information and biological‑assay experimental data of this compound.

Description	X-376 is a potent and dual ALK/MET inhibitor with IC50s of 0.61 nM and 0.69 nM, respectively.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR Research Areas >> Cancer
Target	ALK:0.61 nM (IC50) MET:0.69 nM (IC50)
In Vitro	The ability of X-376 to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. X-376 is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 77 nM). X-376 is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 57 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 32 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 142 nM, 150 nM, 15.137 μM and 3.062 μM, respectively[1].
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].
Cell Assay	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-376 (10, 30, 100, 300 and 1000 nM). SUDHL-1 lymphoma cells are treated with X-376 (5, 10, 30, 100 and 300 nM). SY5Y neuroblastoma cells are treated with X-376 (30, 100, 300 and 1000 nM). At 72 hours post X-376 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].
Animal Admin	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 50 mg/kg X-376 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.
References	[1]. Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31.

This table shows physicochemical parameters including melting point, boiling point, density, solubility and optical rotation. Missing data is marked as N/A.

Density	1.4±0.1 g/cm3
Boiling Point	695.1±55.0 °C at 760 mmHg
Molecular Formula	C₂₅H₂₅Cl₂FN₆O₃
Molecular Weight	547.409
Flash Point	374.2±31.5 °C
Exact Mass	546.134949
PSA	113.68000
LogP	4.21
Vapour Pressure	0.0±2.2 mmHg at 25°C
Index of Refraction	1.654
InChIKey	ONPGOSVDVDPBCY-CQSZACIVSA-N
SMILES	CC(Oc1cc(C(=O)Nc2ccc(C(=O)N3CCN(C)CC3)cc2)nnc1N)c1c(Cl)ccc(F)c1Cl

This table lists upstream starting materials and downstream derivative products related to this chemical.

Precursor 6
CAS#:1370651-39-0 CAS#:756520-66-8 1-(2,6-Dichloro... CAS#:330156-50-8 (R)-1-(2,6-Dich... CAS#:1370651-32-3 (R)-Bi(tert-but...
CAS#:1370651-34-5 6-[Bis[(1,1-diM... CAS#:1370651-36-7 6-[bis(tert-but...
DownStream 0

This table contains target information, in‑vitro & in‑vivo assay data for this compound.

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Aurora kinase A
External Id: CHEMBL3991630

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Breakpoint cluster region protein
External Id: CHEMBL3991632

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Aurora kinase B
External Id: CHEMBL3991631

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Serine/threonine-protein kinase A-Raf
External Id: CHEMBL3991628

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Adenine phosphoribosyltransferase
External Id: CHEMBL3991627

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Tyrosine-protein kinase BTK
External Id: CHEMBL3991638

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Serine/threonine-protein kinase B-raf
External Id: CHEMBL3991637

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Mitotic checkpoint serine/threonine-protein kinase BUB1
External Id: CHEMBL3991639

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: Bone morphogenetic protein receptor type-1A
External Id: CHEMBL3991634

Name: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhib...
Source: ChEMBL
Target: BMP-2-inducible protein kinase
External Id: CHEMBL3991633

Total 285, Current Page 1 of 29

This table collects all English aliases, systematic names and CAS‑related synonyms of the compound.

X-376

UNII-7DR7JMB8BH

X-396

3-Pyridazinecarboxamide,6-amino-5-((1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-N-(4-((4-methyl-1-piperazinyl)carbonyl)phenyl)

{5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-6-aminopyridazin-3-yl}-N-{4-[(4-methylpiperazinyl)carbonyl]phenyl}carboxamide

6-Amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-{4-[(4-methyl-1-piperazinyl)carbonyl]phenyl}-3-pyridazinecarboxamide

(R)-6-Amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-N-(4-(4-methylpiperazine-1-carbonyl)phenyl)pyridazine-3-carboxamide

X 396

Ensartinib

This section contains frequently‑asked‑questions about this compound, including basic parameters, properties, storage conditions and corresponding answers.

Q: What is the English name of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: The English name of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide is 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide.

Q: What is the molecular weight of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: Molecular weight of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide is 547.409.

Q: What is the InChIKey of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: InChIKey of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide is ONPGOSVDVDPBCY-CQSZACIVSA-N.

Q: What is the polar surface area (PSA) of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: Polar surface area (PSA) of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide is 113.68000.

Q: What is the boiling point of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: Boiling point of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide is 695.1±55.0 °C at 760 mmHg.

Q: What is the LogP of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: LogP of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide is 4.21.

Q: What is the molecular formula of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: Molecular formula of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide is C25H25Cl2FN6O3.

Q: What is the CAS number of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: CAS number of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide is 1365267-27-1.

Q: What are the upstream materials of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: Related upstream materials(CAS) of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide: 1370651-39-0;756520-66-8;330156-50-8;1370651-32-3;1370651-34-5;1370651-36-7.

Q: What are the uses of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide?

A: Main uses of 6-amino-5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-[4-(4-methylpiperazine-1-carbonyl)phenyl]pyridazine-3-carboxamide: X-376 is a potent and dual ALK/MET inhibitor with IC50s of 0.61 nM and 0.69 nM, respectively.

This table lists manufacturers and suppliers of this compound, including vendor names and product supply reference information.

Shanghai Nianxing Industrial Co., Ltd

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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Ensartinib
Price: Check
Purity: 98.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

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Price: $405/10mM*1mLinDMSO

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