Sitravatinib malate
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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- No. CAS: 2244864-88-6
- Fòrmula: C37H35F2N5O9S
- Peso molecular:763.76
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Almacenamiento:
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Publications Citing Use of MedChemExpress (MCE) Sitravatinib malate
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Actividad biológica
Descripciòn
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.
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Cell Line:KLN205, E0771, CT1B-A5 cells
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:5 days
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Result:Inhibited KLN205, E0771, CT1B-A5 cells with IC50s of approximately 1 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old C57BL/6 mice (bearing CT1B-A5 cells)[2]
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Dosage:20 mg/kg
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Administration:Oral administration; once per day for 6 days
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Result:Significantly inhibited tumor progression and induced tumor regression.
Chemical Information
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No. CAS 2244864-88-6
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Peso molecular 763.76
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Fòrmula C37H35F2N5O9S
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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
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Synonyms
MGCD516 malate; MG-516 malate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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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
2024 May 8:2024.05.07.592424. PMID: 38766123 -
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sitravatinib malate Related Classifications
HY-16961A Related Classifications
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