Foretinib [849217-64-7]
Cat# HY-10338-50mg
Size : 50mg
Brand : MedChemExpress
Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
For research use only. We do not sell to patients.
Foretinib Chemical Structure
CAS No. : 849217-64-7
This product is a controlled substance and not for sale in your territory.
Based on 12 publication(s) in Google Scholar
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Description |
Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR. |
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IC50 & Target[1] |
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In Vitro |
Foretinib inhibits HGF receptor family tyrosine kinases with IC50 values of 0.4 nM for Met and 3 nM for Ron. Foretinib also inhibits KDR, Flt-1, and Flt-4 with IC50 values of 0.9 nM, 6.8 nM and 2.8 nM, respectively. Foretinib inhibits colony growth of B16F10, A549 and HT29 cells with IC50 of 40 nM, 29 nM and 165 nM, respectively[1].?A recent study indicates Foretinib affects cell growth differently in gastric cancer cell lines MKN-45 and KATO-III. Foretinib inhibits phosphorylation of MET and downstream signaling molecules in MKN-45 cells, while targets GFGR2 in KATO-III cells[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Foretinib (100 mg/kg, p.o.) results in substantial inhibition of phosphorylation of B16F10 tumor Met and ligand (e.g., HGFor VEGF)-induced receptor phosphorylation of Met in liver and Flk-1/KDR in lung, which both persist through 24 hours. Foretinib (30-100 mg/kg, once daily, p.o.) results in reduction in tumor burden. The lung surface tumor burden is reduced by 50% and 58% following treatment with 30 and 100 mg/kg Foretinib, respectively. Foretinib treatment of mice bearing B16F10 solid tumors also results in dose-dependent tumor growth inhibition of 64% and 87% at 30 and 100 mg/kg, respectively. For both studies, administration of Foretinib is well tolerated with no significant body weight loss[1]. Foretinib is developed to target abnormal signaling of HGF through Met and simultaneously target several receptors tyrosine kinase involved in tumor angiogenesis. Foretinib causes tumor hemorrhage and necrosis in human xenografts within 2 to 4 hours, and maximal tumornecrosis is observed at 96 hours (after five daily doses), resulting in complete regression[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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Molecular Weight |
632.65 |
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Formula |
C34H34F2N4O6 |
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CAS No. |
849217-64-7 |
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Appearance |
Solid |
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Color |
White to light yellow |
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SMILES |
O=C(NC1=CC=C(C(F)=C1)OC2=C3C=C(C(OCCCN4CCOCC4)=CC3=NC=C2)OC)C5(CC5)C(NC6=CC=C(C=C6)F)=O |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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Solvent & Solubility |
In Vitro:
DMSO : 75 mg/mL (118.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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).
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.
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Purity & Documentation |
Purity: 99.77% |
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References |
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Complete Stock Solution Preparation Table
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 1.5807 mL | 7.9033 mL | 15.8065 mL | 39.5163 mL |
5 mM | 0.3161 mL | 1.5807 mL | 3.1613 mL | 7.9033 mL | |
10 mM | 0.1581 mL | 0.7903 mL | 1.5807 mL | 3.9516 mL | |
15 mM | 0.1054 mL | 0.5269 mL | 1.0538 mL | 2.6344 mL | |
20 mM | 0.0790 mL | 0.3952 mL | 0.7903 mL | 1.9758 mL | |
25 mM | 0.0632 mL | 0.3161 mL | 0.6323 mL | 1.5807 mL | |
30 mM | 0.0527 mL | 0.2634 mL | 0.5269 mL | 1.3172 mL | |
40 mM | 0.0395 mL | 0.1976 mL | 0.3952 mL | 0.9879 mL | |
50 mM | 0.0316 mL | 0.1581 mL | 0.3161 mL | 0.7903 mL | |
60 mM | 0.0263 mL | 0.1317 mL | 0.2634 mL | 0.6586 mL | |
80 mM | 0.0198 mL | 0.0988 mL | 0.1976 mL | 0.4940 mL | |
100 mM | 0.0158 mL | 0.0790 mL | 0.1581 mL | 0.3952 mL |
Foretinib Related Classifications
- Protein Tyrosine Kinase/RTK
- VEGFR c-Met/HGFR