Elzovantinib (TPX-0022, CSF1rin-2) is a potent MET/CSF1R/SRC inhibitor with IC50 of 0.14 nM, 0.71 nM, and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.

 

Brand: BCM

 

Target: c-Fms; c-Met/HGFR; Src

 

Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors

 

In Vitro: The suppression of MET autophosphorylation as well as the downstream STAT3 caused by CSF1R-IN-2, ERK and AKT phosphorylation at IC50 values of around 1-3 nM in SNU-5 and MKN-45 cell lines.

 

In Vivo: In mice, CSF1R-IN-2 (p.o., BID, 13 days) treatment results in an 85% tumor regression, and no bodyweight loss is observed after 21 days of treatment. In SCID/Beige mice. CSF1R-IN-2 (p.o., BID, 10 days) demonstrates the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID, and 15 mg/kg, BID, respectively. In mice, CSF1R-IN-2 inhibits MET activity in MKN-45 tumors following oral administration.

 

Solubility: Soluble in Ethanol. Insoluble in Water; Insoluble in DMSO.

 

Isomeric SMILES: CCN1CC2=C(C=CC(=C2C#N)F)O[C@H](CNC(=O)C3=C4N=C1C=CN4N=C3N)C  

 

InChIKey: UUDPUQDMSHQSKH-NSHDSACASA-N  

 

InChI: InChI=1S/C20H20FN7O2/c1-3-27-10-13-12(8-22)14(21)4-5-15(13)30-11(2)9-24-20(29)17-18(23)26-28-7-6-16(27)25-19(17)28/h4-7,11H,3,9-10H2,1-2H3,(H2,23,26)(H,24,29)/t11-/m0/s1 

 

Attribute
[Chem Name]	(11S)-16-amino-2-ethyl-6-fluoro-11-methyl-14-oxo-10-oxa-2,13,17,18,21-pentazatetracyclo[13.5.2.04,9.018,22]docosa-1(21),4(9),5,7,15(22),16,19-heptaene-5-carbonitrile
[Synonym]	Elzovantinib; TPX-0022; CSF1R-IN-2
[CAS No.]	2271119-26-5
[MDL No.]	MFCD32062691
[Formula]	C20H20FN7O2
[Molecular]	409.42
[Form]	Solid Powder
[Storage]	Sealed in dry. Stored at -20°C.

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