2. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK
  3. Raf PDGFR FLT3 c-Kit
  4. KG5

KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.

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KG5 Chemical Structure

KG5 Chemical Structure

CAS No. : 877874-85-6

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Based on 1 publication(s) in Google Scholar

KG5 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities[1].

IC50 & Target[1]

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 EC50 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 Kds 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KG5 Related Antibodies
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].

MedChemExpress (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.
Molecular Weight

459.45

Formula

C20H16F3N7OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CSC1=NC(OC2=CC=C(C=C2)C3=NN=C(N3)NC4=CC=CC(C(F)(F)F)=C4)=CC(N)=N1
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
In Vitro: 

DMSO : 100 mg/mL (217.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.79%

SDS (251 KB)

COA (247 KB) LCMS (255 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1765 mL 10.8826 mL 21.7652 mL 54.4129 mL
5 mM 0.4353 mL 2.1765 mL 4.3530 mL 10.8826 mL
10 mM 0.2177 mL 1.0883 mL 2.1765 mL 5.4413 mL
15 mM 0.1451 mL 0.7255 mL 1.4510 mL 3.6275 mL
20 mM 0.1088 mL 0.5441 mL 1.0883 mL 2.7206 mL
25 mM 0.0871 mL 0.4353 mL 0.8706 mL 2.1765 mL
30 mM 0.0726 mL 0.3628 mL 0.7255 mL 1.8138 mL
40 mM 0.0544 mL 0.2721 mL 0.5441 mL 1.3603 mL
50 mM 0.0435 mL 0.2177 mL 0.4353 mL 1.0883 mL
60 mM 0.0363 mL 0.1814 mL 0.3628 mL 0.9069 mL
80 mM 0.0272 mL 0.1360 mL 0.2721 mL 0.6802 mL
100 mM 0.0218 mL 0.1088 mL 0.2177 mL 0.5441 mL
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KG5 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KG5877874-85-6KG 5KG-5RafPDGFRFLT3c-KitRaf kinasesPlatelet-derived growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3SCFRCD117PDGFRβB-RafmetastasisanticancerantiangiogenicphosphorylationFlt3KITc-RafInhibitorinhibitorinhibit

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