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25mg | ||
50mg | ||
100mg | ||
250mg |
Sitravatinib malate (MGCD516) is a novel and potent receptor tyrosine kinase (RTK) inhibitor with anticancer activity and can potentiates immune checkpoint blockade in refractory cancer models. It inhibits Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB 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, respectively.
ln Vitro |
In KLN205 and E0771 cell lines, sitravatinib (0.01 nM–10 μM; 14 days) decreases colony formation in a dose-dependent manner[2]. In KLN205, E0771, and CT1B-A5 cell lines, trastraditinib (0.001–10 μM; 5 days) decreases tumor cell viability with IC50s of roughly 1 μM[2].
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ln Vivo |
In C57BL/6 mice carrying CT1B-A5 cells model, sitravatinib (20 mg/kg; po; once per day for 6 days) effectively suppresses tumor growth and produces tumor regression[2].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: KLN205, E0771, CT1B-A5 cells Tested Concentrations: 0.001, 0.01, 0.1, 1, 10 μM Incubation Duration: 5 days Experimental Results: Inhibited KLN205, E0771, CT1B-A5 cells with IC50s of approximately 1 μM. |
Animal Protocol |
Animal/Disease Models: 6weeks old C57BL/6 mice (bearing CT1B-A5 cells)[2]
Doses: 20 mg/kg Route of Administration: Oral administration; once per day for 6 days Experimental Results: Dramatically inhibited tumor progression and induced tumor regression. |
References |
[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.
[2]. Du W, et al. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018 Nov 2;3(21). pii: 124184. |
Molecular Formula |
C₃₇H₃₅F₂N₅O₉S
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Molecular Weight |
763.76
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CAS # |
2244864-88-6
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Related CAS # |
Sitravatinib;1123837-84-2
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SMILES |
S1C(C2C([H])=C([H])C(=C([H])N=2)C([H])([H])N([H])C([H])([H])C([H])([H])OC([H])([H])[H])=C([H])C2C1=C(C([H])=C([H])N=2)OC1C([H])=C([H])C(=C([H])C=1F)N([H])C(C1(C(N([H])C2C([H])=C([H])C(=C([H])C=2[H])F)=O)C([H])([H])C1([H])[H])=O.O([H])[C@]([H])(C(=O)O[H])C([H])([H])C(=O)O[H]
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Synonyms |
MGCD-516 malateMGCD516 malateSitravatinib malate
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3093 mL | 6.5466 mL | 13.0931 mL | |
5 mM | 0.2619 mL | 1.3093 mL | 2.6186 mL | |
10 mM | 0.1309 mL | 0.6547 mL | 1.3093 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.