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

Sitravatinib malate (Synonyms: MGCD516 malate; MG-516 malate)

Cat. No.: HY-16961A
Handling Instructions

Sitravatinib malate (MGCD516 malate) 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 malate 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 malate Chemical Structure

Sitravatinib malate Chemical Structure

CAS No. : 2244864-88-6

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Description

Sitravatinib malate (MGCD516 malate) 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 malate 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].

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].

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

763.76

Formula

C₃₇H₃₅F₂N₅O₉S

CAS No.

2244864-88-6

SMILES

O=C(O)[[email protected]@H](O)CC(O)=O.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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SitravatinibMGCD516MG-516MGCD 516MGCD-516MG516MG 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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Sitravatinib malate
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HY-16961A
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