| Field | Specification |
|---|---|
| Target | |
| Alternative names | MGCD516 malate; MG-516 malate |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C37H35F2N5O9S |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Sitravatinib malate, also known as MGCD516 malate, is an orally bioavailable inhibitor of receptor tyrosine kinases (RTKs), with IC50 values of 1.5 nM for Axl, 2 nM each for MER and VEGFR3, 5 nM each for VEGFR2 and TRKA, 6 nM each for VEGFR1 and KIT, 8 nM for FLT3, 0.5 nM for DDR2, 29 nM for DDR1, and 9 nM for TRKB[1]. As a single agent, it shows potent antitumor efficacy and boosts the activity of PD-1 blockade by promoting an antitumor immune microenvironment[2]. It has the molecular formula C37H35F2N5O9S and a molecular weight of 763.76 g/mol.
Physical & Chemical Properties
| CAS Number | 2244864-88-6 |
|---|---|
| Molecular Formula | C37H35F2N5O9S |
| Molecular Weight | 763.76 g/mol |
| 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 |
| Target | Axl, MER, VEGFR3, VEGFR2, VEGFR1, TrkA, TrkB, KIT, FLT3, DDR2, DDR1 |
| Signaling Pathway | Protein Tyrosine Kinase/RTK; Neuronal Signaling |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
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) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
In KLN205 and E0771 cell lines, Sitravatinib (0.01 nM-10 μM; 14 days) lowers colony formation in a dose-dependent manner[2]. Sitravatinib (0.001-10 μM; 5 days) reduces tumor cell viability, with IC50s of approximately 1 μM in the 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
In C57BL/6 mice bearing CT1B-A5 cells, Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) produces significant inhibition of tumor progression and causes tumor regression[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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Adiponectin reduces immune checkpoint inhibitor-induced inflammation without blocking anti-tumor immunity. Cancer Cell 2025 Feb 10;43(2):269-291.e19. PMID: 39933899
TNF switches homeostatic efferocytosis to lytic caspase-8-dependent pyroptosis and IL-1β maturation. Sci Immunol 2025 Jun 20;10(108):eadq0043. PMID: 40540586
Blockade of Discoidin Domain Receptor Signaling with Sitravatinib Reveals DDR2 as a Mediator of Neuroblastoma Pathogenesis and Metastasis. Mol Cancer Ther 2024 Aug 1;23(8):1124-1138. PMID: 38670553
PTP1B Modulates Carotid Plaque Vulnerability in Atherosclerosis Through Rab5-PDGFRβ-Mediated Endocytosis Disruption and Apoptosis. CNS Neurosci Ther 2024 Nov;30(11):e70071. PMID: 39517122
Collagen I is a critical organizer of scarring and CNS regeneration failure. bioRxiv 2024 May 8:2024.05.07.592424. PMID: 38766123
SSRN. 2023 Jun 19.
