[CAS NO. 877874-85-6] KG5
PRODUCTS SPECIFICATIONS [877874-85-6]
DESCRIPTION [877874-85-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 459.45 |
| Molecular Formula | C20H16F3N7OS |
| SMILES | CSC1=NC(OC2=CC=C(C=C2)C3=NN=C(N3)NC4=CC=CC(C(F)(F)F)=C4)=CC(N)=N1 |
Summary
IC50 & Target
|
B-Raf
|
PDGFRβ 520 nM (Kd) |
FLT3 52 nM (Kd) |
KIT 170 nM (Kd) |
PDGFRα 300 nM (Kd) |
c-Raf
|
In Vitro
KG5 (Compound 6) inhibits vascular smooth muscle cells (VSMCs) and endothelial cells viability with EC
50
values of 0.59 μM and 0.54 μM, respectively
[1]
.
Compound 6 selectively blocks S338 phosphorylation, yet does not influence S259
[1]
.
KG5 (Compound 6) inhibits only PDGFRα and β with K
d
s of 300 and 520 nM, respectively, and Flt3 and KIT at 52 and 170 nM, respectively
[1]
.
KG5 (Compound 6; 5 μM) inhibits phosphorylation of MEK and ERK in endothelial cells stimulated with bFGF or VEGF
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 C
max
of 3.6 μg/mL, T
1/2
of 11.5 h, and an area under the concentration time curve (AUC
0-12h
) of 14.7 μg•h/mL
[1]
.
KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL ( 217.65 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1765 mL | 10.8826 mL | 21.7652 mL |
| 5 mM | 0.4353 mL | 2.1765 mL | 4.3530 mL |
| 10 mM | 0.2177 mL | 1.0883 mL | 2.1765 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution
Synonyms