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ZM 306416 VEGFR inhibitor

Name: ZM 306416
Brand: Selleck Chemicals
SKU: S2897
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S2897

ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.

Chemical Structure

Molecular Weight: 333.74

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	EGFR PDGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
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Chemical Information, Storage & Stability

Molecular Weight	333.74	Formula	C₁₆H₁₃ClFN₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	690206-97-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CB 676475			Smiles	COC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=C(C=C3)Cl)F)OC

Solubility

In vitro
Batch:

DMSO : 67 mg/mL (200.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.350mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 67 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.600mg/ml (4.79mM)	Taking the 1 mL working solution as an example, add 50 μL of 32 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	VEGFR1 ^[1] 0.33 μM Src ^[1] 0.33 μM Abl ^[1] 1.3 μM
In vitro	ZM-306416 induces selective antiproliferative effect toward the EGFR-addicted NSCLC cell lines H3255 and HCC4011 with IC50 of 0.09 µM and 0.072 µM, respectively. ZM-306416 inhibits granule formation with IC50 of 0.67 μM. ^[1] ZM-306416 significantly inhibits the ERRα assay with IC50 of 7.3 μM in the GeneBLAzer T-Rex RORγ-UAS-bla HEK293T cell line. ^[2] ZM306416 (300 nM) completely inhibits PAA secretion and stimulates [¹²⁵]I uptake in human thyroid follicular cells. ZM306416 (300 nM) abolishes pVEGFR2 (Y1214) expression in human thyroid follicular cells. ZM306416 (< 10 μM) has marked inhibitory effects on the steady state phosphorylation of p42/44 MAPK but does not affect the expression of the unphosphorylated form. ZM306416 (3 μM) significantly increases cell death in human thyroid follicular cells. ZM306416 (3 μM) significantly increases cell death in human thyroid follicular cells. ZM306416 weakly inhibits the secretion of VEGF and increases the production of PlGF. ^[3] ZM306416 (1 μM) enhances follicle formation and decreased nuclear distribution in human thyroid follicular cells. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/22573732/ [2] https://pubmed.ncbi.nlm.nih.gov/21050030/ [3] https://pubmed.ncbi.nlm.nih.gov/22227235/ [4] https://pubmed.ncbi.nlm.nih.gov/21751212/

Tech Support

Handling Instructions

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