KG5
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.79%
- CAS No.: 877874-85-6
- Formula: C20H16F3N7OS
- Molecular Weight:459.45
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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B-Raf |
PDGFRβ 520 nM (Kd) |
FLT3 52 nM (Kd) |
KIT 170 nM (Kd) |
PDGFRα 300 nM (Kd) |
C-Raf |
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 (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.
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Animal Model:Male Nu/Nu mice injected with SN12C-RFP cells[1]
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Dosage:100 mg/kg
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Administration:Oral administration; daily; for 26 days
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Result:Prevented tumor growth in an orthotopic renal cell carcinoma model.
Chemical Information
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CAS No. 877874-85-6
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Appearance Solid
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Molecular Weight 459.45
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Formula C20H16F3N7OS
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Color White to off-white
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SMILES
CSC1=NC(OC2=CC=C(C=C2)C3=NN=C(N3)NC4=CC=CC(C(F)(F)F)=C4)=CC(N)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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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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