Orantinib (TSU-68, SU6668) is potent on PDGFR autophosphorylation with Ki of 8 nM in cell-free assay. It also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, and has significant effects on IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 had little inhibitory activity. There was no inhibitory effect on EGFR. Phase 3.

 

Brand: BCM

 

Target: Apoptosis; VEGFR; FGFR; PDGFR

 

Signaling Pathways: Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors

 

In Vitro: In the HT29 human colon cancer tumor model,TSU-68 (200 mg/kg) reduced the mean vascular permeability at the tumor edge and the mean plasma volume fraction at the tumor center. TSU-68 (75-200 mg/kg) inhibited tumor growth in athimic mice bearing multiple tumor xenografts, including A375,Colo205,H460,Calu-6,C6,SF763T, and SKOV3TP5 cells. In the rabbit VX2 liver tumor model, TSU-68 (200 mg/kg) increased the efficacy of injection chemotherapy. In C6 glial cell xenografts, TSU-68 (75 mg/kg) also blocked tumor angiogenesis.

 

Melting Point: 252-254 °C

 

Boiling Point: 590.5±50.0 °C(Predicted)

 

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

 

GHS: GHS05, GHS06, GHS08

 

Isomeric SMILES: CC1=C(NC(=C1CCC(=O)O)C)/C=C\2/C3=CC=CC=C3NC2=O  

 

InChIKey: NHFDRBXTEDBWCZ-ZROIWOOFSA-N  

 

InChI: InChI=1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9- 

 

Attribute
[Chem Name]	3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
[Synonym]	Orantinib; SU6668; TSU-68
[CAS No.]	252916-29-3
[MDL No.]	MFCD03426212
[Formula]	C18H18N2O3
[Molecular]	310.35
[Form]	Orange to Brown Solid
[Storage]	Sealed in dry. Store in freezer, under -20°C

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