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Art. -Nr.: HY-16961A

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Sitravatinib malate

(Synonyms: MGCD516 malate; MG-516 malate)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

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.

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CAS. Nr.: 2244864-88-6
Formel: C₃₇H₃₅F₂N₅O₉S
Molecular Weight:763.76

Speicherung:

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

Data Sheet (273 KB)

Sitravatinib malate Chemical Structure

CAS. Nr.: 2244864-88-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen :

DDR1
DDR2

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 2244864-88-6
Molecular Weight 763.76
Formel C₃₇H₃₅F₂N₅O₉S
SMILES

O=C(O)[C@@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
Synonyms

MGCD516 malate; MG-516 malate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Publications (6)

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Journal Impact Factor

Cancer Cell

Adiponectin reduces immune checkpoint inhibitor-induced inflammation without blocking anti-tumor immunity. [Abstract]

2025 Feb 10;43(2):269-291.e19. PMID: 39933899
Sci Immunol

TNF switches homeostatic efferocytosis to lytic caspase-8-dependent pyroptosis and IL-1β maturation. [Abstract]

2025 Jun 20;10(108):eadq0043. PMID: 40540586
Mol Cancer Ther

Blockade of Discoidin Domain Receptor Signaling with Sitravatinib Reveals DDR2 as a Mediator of Neuroblastoma Pathogenesis and Metastasis. [Abstract]

2024 Aug 1;23(8):1124-1138. PMID: 38670553
CNS Neurosci Ther

PTP1B Modulates Carotid Plaque Vulnerability in Atherosclerosis Through Rab5-PDGFRβ-Mediated Endocytosis Disruption and Apoptosis. [Abstract]

2024 Nov;30(11):e70071. PMID: 39517122
bioRxiv

Collagen I is a critical organizer of scarring and CNS regeneration failure. [Abstract]

2024 May 8:2024.05.07.592424. PMID: 38766123
SSRN

2023 Jun 19.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109. [Content Brief]

[2]. Du W, et al. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018 Nov 2;3(21). pii: 124184. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Sitravatinib malate

6 Cited Publications

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

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CAS. Nr.:
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Sitravatinib malate

Publications Citing Use of MedChemExpress (MCE) Sitravatinib malate

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Sitravatinib malate Related Classifications

HY-16961A Related Classifications