GSK3179106 is a potent and selective inhibitor of RET (c-RET) kinase with an IC50 of 0.3 nM.

 

Brand: BCM

 

Target: c-RET

 

Signaling Pathways: Apoptosis; Tyrosine Kinase/Adaptors

 

In Vitro: The effect of GSK3179106 on human and rat RET enzymatic activity and motesanib on human RET enzymatic activity was determined in an in vitro biochemical homogeneous time-resolved fluorescence (HTRF) assay.

 

In Vivo: GSK3179106 (3 or 10 mg/kg; orally; for 3.5 days BID) reduces the visceromotor response (VMR) in comparison to rats given an acetic acid enema and dosed with vehicle.

 

Boiling Point: 670.1±55.0 °C(Predicted)

 

pKa: 10.30±0.10(Predicted)

 

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

 

GHS: GHS07

 

Isomeric SMILES: CCOC1=CC(=O)NC=C1C2=CC(=C(C=C2)CC(=O)NC3=NOC(=C3)C(C)(C)C(F)(F)F)F

 

InChIKey: IDXKJSSOUXWLDB-UHFFFAOYSA-N

 

InChI: InChI=1S/C22H21F4N3O4/c1-4-32-16-9-19(30)27-11-14(16)12-5-6-13(15(23)7-12)8-20(31)28-18-10-17(33-29-18)21(2,3)22(24,25)26/h5-7,9-11H,4,8H2,1-3H3,(H,27,30)(H,28,29,31)

 

Attribute
[CAS No.]	1627856-64-7
[Formula]	C22H21F4N3O4
[Molecular]	467.4134528
[Chem Name]	2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]acetamide
[Synonym]	RET Kinase inhibitor 1; GSK3179106
[Storage]	Sealed in dry, 2-8°C
[MDL No.]	MFCD30747847
[Form]	A crystalline solid

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