Art. -Nr.: HY-13785

ZM 306416

(Synonyms: CB 676475)

2 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.80%
CAS. Nr.: 690206-97-4
Formel: C₁₆H₁₃ClFN₃O₂
Molecular Weight:333.75

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ZM 306416 Chemical Structure

CAS. Nr.: 690206-97-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target^[1]

KDR

100 nM (IC₅₀)

Flt-1

2 μM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A498	IC₅₀	14.1 μM Compound: 14, CB-676475	Inhibition of VEGFR1 in human A498 cells by phosphotyrosine cell-based ELISA Inhibition of VEGFR1 in human A498 cells by phosphotyrosine cell-based ELISA	[PMID: 20092323]
A498	IC₅₀	14.1 μM Compound: 19, CB676475	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	[PMID: 22204741]
A498	IC₅₀	14.1 μM Compound: 26, CB676475	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	[PMID: 23375090]
A498	IC₅₀	14.1 μM Compound: 48, CB-676475	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	[PMID: 20403700]
A498	IC₅₀	17.7 μM Compound: 21, CB-676475	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	[PMID: 22370340]

In Vitro

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

CAS. Nr. 690206-97-4
Appearance Solid
Molecular Weight 333.75
Formel C₁₆H₁₃ClFN₃O₂
Color White to gray
SMILES

COC1=CC2=NC=NC(NC3=C(F)C=C(Cl)C=C3)=C2C=C1OC
Synonyms

CB 676475
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

J Neurosci

Growth Factor Signaling Regulates Mechanical Nociception in Flies and Vertebrates. [Abstract]

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9963 mL

14.9813 mL

29.9625 mL

5 mM

0.5993 mL

2.9963 mL

5.9925 mL

10 mM

0.2996 mL

1.4981 mL

2.9963 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (7.49 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

ZM 306416

2 Cited Publications

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ZM 306416

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MCE Kinase Hinge Binder Fragment Library

Publications Citing Use of MedChemExpress (MCE) ZM 306416

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ZM 306416

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MCE Kinase Hinge Binder Fragment Library

Publications Citing Use of MedChemExpress (MCE) ZM 306416

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ZM 306416 Related Classifications

HY-13785 Related Classifications