GW768505A free base

Name: GW768505A free base
Brand: MedChemExpress
SKU: HY-125741
Rating: 4.5 (1 reviews)

Cat. No.: HY-125741 Purity: 98.66%: FAQs
Data Sheet SDS COA Handling Instructions

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GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC₅₀ of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity。

For research use only. We do not sell to patients.

GW768505A free base Chemical Structure

CAS No. : 501693-25-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 260	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 260	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Tie Isoform Specific Products:

View All Isoforms

Tie2

View All VEGFR Isoform Specific Products:

View All Isoforms

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Biological Activity
Purity & Documentation
References
Customer Review

Description

GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC₅₀ of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity^[1]。

IC₅₀ & Target^[1]

KDR

Tie2

Tie-2

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	0.045 μM Compound: 7k	Concentration required for growth inhibition of human umbilical vein endothelial cells stimulated by VEGF Concentration required for growth inhibition of human umbilical vein endothelial cells stimulated by VEGF	[PMID: 15837294]

In Vitro

GW768505A free base has inhibition for cancer cells growth in NCI-60 panel screening^[2].
GW768505A free base is an inhibitor of KDR and TIE2, shows potent inhibition (71–88% inhibition at 100 nM) of the tropomysin-related kinases TRKA, TRKB and TRKC^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

537.47

Formula

C₂₇H₁₉F₄N₅O₃

CAS No.

501693-25-0

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C3=C(C4=CC=C(OC)C=C4)OC5=NC=NC(N)=C53)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 8.33 mg/mL (15.50 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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8606 mL	9.3028 mL	18.6057 mL
5 mM	0.3721 mL	1.8606 mL	3.7211 mL
10 mM	0.1861 mL	0.9303 mL	1.8606 mL

View the 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.

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Dilution Calculator

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

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Concentration _(final)

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In Vivo Dissolution Calculator

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.66%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (259 KB) HNMR (143 KB) RP-HPLC (152 KB) LCMS (231 KB)

Handling Instructions (2659 KB)

References

[1]. Miyazaki Y, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8. [Content Brief]

[2]. Elkins JM, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016 Jan;34(1):95-103. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8606 mL	9.3028 mL	18.6057 mL	46.5142 mL
	5 mM	0.3721 mL	1.8606 mL	3.7211 mL	9.3028 mL
	10 mM	0.1861 mL	0.9303 mL	1.8606 mL	4.6514 mL
	15 mM	0.1240 mL	0.6202 mL	1.2404 mL	3.1009 mL