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KG5

🥰Excellent
Catalog No. T41003Cas No. 877874-85-6

KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.

KG5

KG5

🥰Excellent
Purity: 98.2%
Catalog No. T41003Cas No. 877874-85-6
KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.
Pack SizePriceAvailabilityQuantity
1 mg$29In Stock
2 mg$39In Stock
5 mg$68In Stock
10 mg$107In Stock
25 mg$215In Stock
50 mg$329In Stock
100 mg$473In Stock
200 mg$662In Stock
1 mL x 10 mM (in DMSO)$82In Stock
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Purity:98.2%
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Product Introduction

Bioactivity
Description
KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.
Targets&IC50
c-Kit:170 nM (Kd), FLT3:52 nM (Kd), PDGFRα:300 nM (Kd), PDGFRβ:520 nM (Kd)
In vitro
KG5 inhibits FLT3 and KIT at 52 and 170 nM, respectively. In endothelial cells stimulated with bFGF or VEGF, KG5 (5 μM) inhibits phosphorylation of MEK and ERK. KG5 inhibits vascular smooth muscle cells (VSMCs) and endothelial cell viability with EC50 values of 0.59 μM and 0.54 μM, respectively. KG5 selectively blocks S338 phosphorylation, yet does not influence S259[1].
In vivo
KG5 (1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis. In male Nu/Nu mice injected with SN12C-RFP cells, KG5 (100 mg/kg; oral) prevents tumor growth. KG5 (50 mg/kg; i.p.) completely blocks angiogenesis in mice injected with Matrigel containing bFGF with a Cmax of 3.6 μg/mL, T1/2 of 11.5 h, and an AUC0-12h of 14.7 μg•h/mL[1].
Chemical Properties
Molecular Weight459.45
FormulaC20H16F3N7OS
Cas No.877874-85-6
SmilesCSc1nc(N)cc(Oc2ccc(cc2)-c2nnc(Nc3cccc(c3)C(F)(F)F)[nH]2)n1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 95 mg/mL (206.77 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1765 mL10.8826 mL21.7652 mL108.8258 mL
5 mM0.4353 mL2.1765 mL4.3530 mL21.7652 mL
10 mM0.2177 mL1.0883 mL2.1765 mL10.8826 mL
20 mM0.1088 mL0.5441 mL1.0883 mL5.4413 mL
50 mM0.0435 mL0.2177 mL0.4353 mL2.1765 mL
100 mM0.0218 mL0.1088 mL0.2177 mL1.0883 mL

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