Sitravatinib malate

Name: Sitravatinib malate
Brand: TargetMol
SKU: T12925
Rating: 4.5 (1 reviews)

😃Good

Catalog No. T12925Cas No. 2244864-88-6

Alias MGCD516 malate, MG-516 malate

Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

Sitravatinib malate

😃Good

Catalog No. T12925Alias MGCD516 malate, MG-516 malateCas No. 2244864-88-6

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	1-2 weeks	1-2 weeks
50 mg	$1,980	1-2 weeks	1-2 weeks
100 mg	$2,500	1-2 weeks	1-2 weeks

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Resource Download

Product Introduction

Bioactivity

Description	Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
Targets&IC50	Mer:2 nM, DDR1:29 nM, FLT3:8 nM, c-Kit:6 nM, Axl:1.5 nM, VEGFR3:2 nM, TrkA:5 nM, VEGFR2:5 nM, VEGFR1:6 nM, TrkB:9 nM, DDR2:0.5 nM
In vitro	In KLN205 and E0771 cell lines,Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner [2]. Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability(IC50s : 1 μM, in KLN205), E0771 and CT1B-A5 cell lines[2].
In vivo	In C57BL/6 mice bearing CT1B-A5 cells model,Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression [2].
Synonyms	MGCD516 malate, MG-516 malate

Chemical Properties

Molecular Weight	763.76
Formula	C₃₇H₃₅F₂N₅O₉S
Cas No.	2244864-88-6
Smiles	[C@H](CC(O)=O)(C(O)=O)O.C(NC1=CC(F)=C(OC2=C3C(C=C(S3)C4=CC=C(CNCCOC)C=N4)=NC=C2)C=C1)(=O)C5(C(NC6=CC=C(F)C=C6)=O)CC5
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc