ZM 306416
Based on 2 publication(s) in Google Scholar
ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.80%
- CAS No.: 690206-97-4
- Formule: C16H13ClFN3O2
- Masse moléculaire:333.75
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Kinase Inhibitor Library
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Publications Citing Use of MedChemExpress (MCE) ZM 306416
MoreVoir tous les produits spécifiques à Isoform VEGFR
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Activité biologique
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KDR 100 nM (IC50) |
Flt-1 2 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A498 | IC50 |
14.1 μM
Compound: 14, CB-676475
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Inhibition of VEGFR1 in human A498 cells by phosphotyrosine cell-based ELISA
Inhibition of VEGFR1 in human A498 cells by phosphotyrosine cell-based ELISA
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[PMID: 20092323] |
| A498 | IC50 |
14.1 μM
Compound: 19, CB676475
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Inhibition of VEGFR1 tyrosine kinase activity in VEGF-stimulated human A498 cells after 60 mins by ELISA
Inhibition of VEGFR1 tyrosine kinase activity in VEGF-stimulated human A498 cells after 60 mins by ELISA
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[PMID: 22204741] |
| A498 | IC50 |
14.1 μM
Compound: 26, CB676475
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Inhibition of VEGF-induced VEGFR1 phosphorylation in human A498 cells overexpressing Flt-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
Inhibition of VEGF-induced VEGFR1 phosphorylation in human A498 cells overexpressing Flt-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
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[PMID: 23375090] |
| A498 | IC50 |
14.1 μM
Compound: 48, CB-676475
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Inhibition of VEGFR1 phosphorylation in human A498 cells after 10 mins by FLISA
Inhibition of VEGFR1 phosphorylation in human A498 cells after 10 mins by FLISA
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[PMID: 20403700] |
| A498 | IC50 |
17.7 μM
Compound: 21, CB-676475
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Inhibition of VEGF-induced VEGFR1 autophosphorylation in human A498 cells incubated for 60 mins prior to VEGF-induction measured after 10 mins by phosphotyrosine ELISA
Inhibition of VEGF-induced VEGFR1 autophosphorylation in human A498 cells incubated for 60 mins prior to VEGF-induction measured after 10 mins by phosphotyrosine ELISA
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[PMID: 22370340] |
ZM-306416 selective anti-proliferative effect toward the EGFR addicted NSCLC cell lines H3255 and HCC4011 (IC50=0.09±0.007 μM and 0.072±0.001 μM respectively), while sparing the wild type EGFR cell lines A549 and H2030 (IC50>10 μM). ZM-306416 is also found to inhibit the ABL in vitro kinase activity with a less potent IC50 value of 1.3±0.2 μM toward the ABL kinase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 690206-97-4
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Appearance Solid
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Masse moléculaire 333.75
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Formule C16H13ClFN3O2
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Color White to gray
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SMILES
COC1=CC2=NC=NC(NC3=C(F)C=C(Cl)C=C3)=C2C=C1OC
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Synonyms
CB 676475
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Neurosci
2019 Jul 24;39(30):6012-6030. PMID: 31138657 -
J Cell Biochem
Vascular endothelial growth factor enhances tendon-bone healing by activating Yes-associated protein for angiogenesis induction and rotator cuff reconstruction in rats. [Abstract]2020 Mar;121(3):2343-2353. PMID: 31633245
Solvant et solubilité
DMSO : 50 mg/mL (149.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (7.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Han SY, Park SS, Lee WG, Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jan 1;16(1):129-33. [Content Brief]
[2]. Antczak C, Mahida JP, Bhinder B, A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen. 2012 Aug;17(7):885-99. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9963 mL | 14.9813 mL | 29.9625 mL | 74.9064 mL |
| 5 mM | 0.5993 mL | 2.9963 mL | 5.9925 mL | 14.9813 mL | |
| 10 mM | 0.2996 mL | 1.4981 mL | 2.9963 mL | 7.4906 mL | |
| 15 mM | 0.1998 mL | 0.9988 mL | 1.9975 mL | 4.9938 mL | |
| 20 mM | 0.1498 mL | 0.7491 mL | 1.4981 mL | 3.7453 mL | |
| 25 mM | 0.1199 mL | 0.5993 mL | 1.1985 mL | 2.9963 mL | |
| 30 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 2.4969 mL | |
| 40 mM | 0.0749 mL | 0.3745 mL | 0.7491 mL | 1.8727 mL | |
| 50 mM | 0.0599 mL | 0.2996 mL | 0.5993 mL | 1.4981 mL | |
| 60 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2484 mL | |
| 80 mM | 0.0375 mL | 0.1873 mL | 0.3745 mL | 0.9363 mL | |
| 100 mM | 0.0300 mL | 0.1498 mL | 0.2996 mL | 0.7491 mL |
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