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Purity: ≥98%
Sitravatinib (formerly known as MGCD516; MG516) is a novel and potent multi-kinase inhibitor targeting multiple RTKs (Receptor tysosine kinases) such as c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl with potential anticancer activity. It suppresses kinases that exhibit low nanomolar activity (less than 10 nM). When administered in vitro, sitravatinib significantly inhibited the phosphorylation of putative driver RTKs and produced strong anti-proliferative outcomes. The application of sitravatinib to tumor xenografts in vivo led to a notable inhibition of tumor growth. Further clinical development of MGCD516 for the treatment of patients with soft-tissue sarcoma is justified by the study's results, which demonstrate blockade of multiple driver signaling pathways.
| Targets |
Axl (IC50 = 1.5 nM); MER (IC50 = 2 nM); VEGFR3 (IC50 = 2 nM); VEGFR2 (IC50 = 5 nM); VEGFR1 (IC50 = 6 nM); TrkA (IC50 = 5 nM); TrkB (IC50 = 9 nM); KIT (IC50 = 64 nM); FLT3 (IC50 = 8 nM); DDR2 (IC50 = 0.5 nM); DDR1 (IC50 = 29 nM)
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| ln Vitro |
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| Enzyme Assay |
Sitravatinib (formerly known as MGCD516 or MG516) is a novel small molecule inhibitor that targets several different RTKs, including Axl, c-Met, PDGFRβ, PDGFRβ, and c-Kit.
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| Cell Assay |
The following day, the prescribed medications were administered to 2,000–3,000 cells that had been plated in 96-well plates using RPMI/DME media containing 10% FBS. The media was changed after 72 hours to 100 μL containing 10% serum and 10% CCK-8 solution. To assess viability, the optical density at 450 nm was measured an hour later. For the final sample quantification, background values from cell-free negative control wells were subtracted. In comparison to the DMSO control, the data was plotted as a percentage of cell viability. Using CompuSyn software and following the manufacturer's instructions, the IC50 was extrapolated from cell viability data.
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| Animal Protocol |
ICR/SCID mice
15 mg/kg p.o. |
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| References |
| Molecular Formula |
C33H29F2N5O4S
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| Molecular Weight |
629.68
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| Exact Mass |
629.19
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| Elemental Analysis |
C, 62.95; H, 4.64; F, 6.03; N, 11.12; O, 10.16; S, 5.09
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| CAS # |
1123837-84-2
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| Related CAS # |
Sitravatinib malate;2244864-88-6
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| Appearance |
Solid powder
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| SMILES |
COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
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| InChi Key |
WLAVZAAODLTUSW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H29F2N5O4S/c1-43-15-14-36-18-20-2-8-25(38-19-20)29-17-26-30(45-29)28(10-13-37-26)44-27-9-7-23(16-24(27)35)40-32(42)33(11-12-33)31(41)39-22-5-3-21(34)4-6-22/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42)
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| Chemical Name |
1-N'-[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.75 mg/mL (4.37 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (3.97 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (3.97 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: ≥ 2.5 mg/mL (3.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1588 mL | 0.7941 mL | 1.5881 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02978859 | Active Recruiting |
Drug: MGCD516 | Liposarcoma Metastatic Liposarcoma |
Matthew Ingham | November 2016 | Phase 2 |
| NCT05407519 | Recruiting | Drug: Tislelizumab + Sitravatinib | Hepatocellular Carcinoma | Anhui Provincial Hospital | July 25, 2022 | Phase 2 |
| NCT04727996 | Active Recruiting |
Drug: Sitravatinib Drug: Tislelizumab |
Advanced Biliary Tract Cancer | Seoul National University Hospital | November 1, 2020 | Phase 2 |
| NCT03906071 | Active Recruiting |
Drug: Sitravatinib Drug: Docetaxel |
Metastatic Non-Squamous Non- Small Cell Lung Cancer |
Mirati Therapeutics Inc. | July 15, 2019 | Phase 3 |
| NCT04925986 | Active Recruiting |
Drug: Sitravatinib Drug: Pembrolizumab |
Lung Diseases Sitravatinib |
Sarah Goldberg | February 10, 2022 | Phase 2 |
 MGCD516 treatment results in superior anti-proliferative effect, better inhibition of downstream targets such as p-AKT and greater reduction in colony growth when compared to imatinib and crizotinib.Oncotarget. 2016 Jan 26; 7(4): 4093–4109. |
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 siRNA mediated knockdown of potential driver RTKs results in inhibition of cell proliferation similar to MGCD516 treatment.Oncotarget. 2016 Jan 26; 7(4): 4093–4109. |
 MGCD516 treatment induces significant suppression of tumor growth and better inhibition of downstream targets than imatinib and crizotinibin vivo.Oncotarget. 2016 Jan 26; 7(4): 4093–4109. |
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