2. Protein Tyrosine Kinase/RTK Neuronal Signaling
  3. VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor
  4. Sitravatinib

Sitravatinib  (Synonyms: MGCD516; MG-516)

Cat. No.: HY-16961 Purity: 99.57%
COA Handling Instructions

Molarity Calculator

Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with 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. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

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

Sitravatinib Chemical Structure

Sitravatinib Chemical Structure

CAS No. : 1123837-84-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Sitravatinib:

Sitravatinib Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All Discoidin Domain Receptor Isoform Specific Products:

View All Isoforms
DDR1 DDR2

View All Trk Receptor Isoform Specific Products:

View All Isoforms
TrkA TrkB TrkC Trk

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with 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[1]. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment[2].

IC50 & Target[1]

Axl

1.5 nM (IC50)

MER

2 nM (IC50)

VEGFR3

2 nM (IC50)

VEGFR2

5 nM (IC50)

VEGFR1

6 nM (IC50)

TrkA

5 nM (IC50)

TrkB

9 nM (IC50)

KIT

6 nM (IC50)

FLT3

8 nM (IC50)

DDR2

0.5 nM (IC50)

DDR1

29 nM (IC50)

In Vitro

Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines[2].
Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability with IC50s of approximately 1 μM in KLN205, E0771 and CT1B-A5 cell lines[2].

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

Sitravatinib Related Antibodies

Cell Viability Assay[2]

Cell Line: KLN205, E0771, CT1B-A5 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 5 days
Result: Inhibited KLN205, E0771, CT1B-A5 cells with IC50s of approximately 1 μM.
In Vivo

Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model[2].

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

Animal Model: 6-week-old C57BL/6 mice (bearing CT1B-A5 cells) [2]
Dosage: 20 mg/kg
Administration: Oral administration; once per day for 6 days
Result: Significantly inhibited tumor progression and induced tumor regression.
Clinical Trial
Molecular Weight

629.68

Formula

C33H29F2N5O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=C5C(C=C(C6=NC=C(CNCCOC)C=C6)S5)=NC=C4)C(F)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (50.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5881 mL 7.9405 mL 15.8811 mL
5 mM 0.3176 mL 1.5881 mL 3.1762 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 2.75 mg/mL (4.37 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (3.97 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.57%

COA (246 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5881 mL 7.9405 mL 15.8811 mL 39.7027 mL
5 mM 0.3176 mL 1.5881 mL 3.1762 mL 7.9405 mL
10 mM 0.1588 mL 0.7941 mL 1.5881 mL 3.9703 mL
15 mM 0.1059 mL 0.5294 mL 1.0587 mL 2.6468 mL
20 mM 0.0794 mL 0.3970 mL 0.7941 mL 1.9851 mL
25 mM 0.0635 mL 0.3176 mL 0.6352 mL 1.5881 mL
30 mM 0.0529 mL 0.2647 mL 0.5294 mL 1.3234 mL
40 mM 0.0397 mL 0.1985 mL 0.3970 mL 0.9926 mL
50 mM 0.0318 mL 0.1588 mL 0.3176 mL 0.7941 mL
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Sitravatinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sitravatinib1123837-84-2MGCD516 MG-516MGCD 516MGCD-516MG516MG 516MG-516VEGFRc-KitFLT3Discoidin Domain ReceptorTrk ReceptorVascular endothelial growth factor receptorSCFRCD117Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Tropomyosin related kinase receptorRTKTyrosinekinaseCancerimmunotherapyMacrophagesimmunePD-1AxlMERVEGFR3VEGFR2VEGFR1KITDDR2DDR1TRKATRKBInhibitorinhibitorinhibit

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