| Identification | Back Directory | [Name]
KG5 | [CAS]
877874-85-6 | [Synonyms]
KG5
2-methylsulfanyl-6-[4-[3-[3-(trifluoromethyl)anilino]-1H-1,2,4-triazol-5-yl]phenoxy]pyrimidin-4-amine
2-(Methylthio)-6-[4-[5-[[3-(trifluoromethyl)phenyl]amino]-1H-1,2,4-triazol-3-yl]phenoxy]-4-pyrimidinamine
4-Pyrimidinamine, 2-(methylthio)-6-[4-[5-[[3-(trifluoromethyl)phenyl]amino]-1H-1,2,4-triazol-3-yl]phenoxy]-
B-Raf,antiangiogenic,KIT,c-Kit,KG5,CD135,Raf kinases,Raf,PDGFR,Cluster of differentiation antigen 135,Platelet-derived growth factor receptor,Fms like tyrosine kinase 3,metastasis,c-Raf,FLT3,PDGFRβ,inhibit,anticancer,phosphorylation,SCFR,Inhibitor,KG 5,CD117,KG-5 | [Molecular Formula]
C20H16F3N7OS | [MDL Number]
MFCD22124522 | [MOL File]
877874-85-6.mol | [Molecular Weight]
459.45 |
| Chemical Properties | Back Directory | [Boiling point ]
654.0±65.0 °C(Predicted) | [density ]
1.54±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
9.54±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
KG 5 is orally active drug that stabilizes inactive state of PDGFRβ/B-RAF and inhibits tumor angiogenesis. | [in vivo]
KG5 (Compound 6; 100 mg/kg; oral administration; daily; for 26 days) treatment prevents tumor growth in an orthotopic renal cell carcinoma model[1].
KG5 (Compound 6; 50 mg/kg; i.p.; twice daily) treatment completely blocks angiogenesis relative to vehicle control in mice (injected with Matrigel containing bFGF). Pharmacokinetic analysis of the dose and formulation of KG5 used indicated a Cmax of 3.6 μg/mL, T1/2 of 11.5 h, and an area under the concentration time curve (AUC0-12h) of 14.7 μg?h/mL[1].
KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis[1]. | Animal Model: | Male Nu/Nu mice injected with SN12C-RFP cells[1] | | Dosage: | 100 mg/kg | | Administration: | Oral administration; daily; for 26 days | | Result: | Prevented tumor growth in an orthotopic renal cell carcinoma model.
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| [IC 50]
B-Raf; PDGFRβ: 520 nM (Kd); FLT3: 52 nM (Kd); KIT: 170 nM (Kd); PDGFRα: 300 nM (Kd); c-Raf | [storage]
Store at -20°C |
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| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
R&D Systems, Inc
|
| Tel: |
18003437475 18003437475 |
| Website: |
www.rndsystems.com |
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