Velzatinib
Based on 1 publication(s) in Google Scholar
Velzatinib (M4205) is a multi-target inhibitor for PDGFRB, PDGFRA, CSF1R, c-Kit, FLT3, and LCK, with an IC50s of 2.6, 50, 5.5, 44, 141 and 141 nM, respectively. Velzatinib exhibits antitumor efficacy in xenograft mouse models.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.40%
- No. CAS: 2590556-80-0
- Fòrmula: C29H32N8O
- Peso molecular:508.62
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Reprogramming Compound Library
HY-L039
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Angiogenesis-Related Compound Library
HY-L088
-
Targeted Diversity Library
HY-L099
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Heterocyclic Compound Library
HY-L138
-
Pain-Related Compound Library
HY-L139
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Cytokine Inhibitors Library
HY-L161
-
Anti-Hematopathy Compound Library
HY-L171
-
Macrophage Related Compound Library
HY-L174
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Anti-Fibrosis Compound Library
HY-L185
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) Velzatinib
More
Actividad biológica
|
PDGFRβ 2.6 nM (IC50) |
CSF1R 5.5 nM (IC50) |
KIT 44 nM (IC50) |
PDGFRA 50 nM (IC50) |
Lck 141 nM (IC50) |
FLT3 141 nM (IC50) |
Velzatinib (M4205) (1 nM-10 μM) inhibits the KIT autophosphorylation in Imatinib (HY-15463) sensitive cell GIST430, Imatinib (HY-15463)-resistant cell line GIST430/654 (exon 11 and exon 13 mutation) and AML cell line Kasumi-1 (exon 17 mutation) with IC50 of 4, 48 and 4 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:GIST430/654 xenograft models[1].
-
Dosage:35 mg/kg
-
Administration:30 days
-
Result:Inhibited tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 2590556-80-0
-
Appearance Solid
-
Peso molecular 508.62
-
Fòrmula C29H32N8O
-
Color White to light brown
-
SMILES
CN1N=CC(C2=CC=C(CNC3=NC=NC(C4=CN=C5C=C(C=CN54)OCCCN6CCCC6)=C3)C=C2)=C1
-
Synonyms
M4205; IDRX-42
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
Solvente y solubilidad
DMSO : 4 mg/mL (7.86 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.4 mg/mL (0.79 mM); Clear solution
This protocol yields a clear solution of ≥ 0.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.4 mg/mL (0.79 mM); Suspended solution
This protocol yields a suspended solution of ≥ 0.4 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
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.
Pureza y Documentación
-
Ficha de datos (272 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 1.9661 mL | 9.8305 mL | 19.6610 mL | 49.1526 mL |
| 5 mM | 0.3932 mL | 1.9661 mL | 3.9322 mL | 9.8305 mL |
Velzatinib Related Classifications
HY-132166 Related Classifications
Powered by Bioz