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S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $78 | In Stock | In Stock | |
| 5 mg | $147 | In Stock | In Stock | |
| 10 mg | $247 | - | In Stock | |
| 25 mg | $446 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $225 | - | In Stock |
| Description | S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM. |
| Targets&IC50 | HCC1143 cells:3.1 ± 0.5 μM (EC50), MDA-MB-468 cells:141.2 ± 24.7 nM (EC50), HH cells:22 nM (EC50), MCL1:0.19 nM (Kd), HuT78 cells:110 nM (EC50) |
| In vitro | METHODS: HCT-116 cells were treated with S63845 (0.001-10 μM), and the levels of MCL1 and BCL-XL proteins in the cells were analyzed by Western blot. RESULTS S63845 effectively increased the level of MCL1 protein in the HCT-116 colon cancer cell line, but had no effect on the level of BCL-XL protein. The increase in MCL1 protein level was not accompanied by an increase in MCL1 mRNA level, but was associated with a prolonged protein half-life. [1] |
| In vivo | METHODS: S63845 (6.25, 12.5, 25 mg/kg, intravenous injection) was used to treat immunocompromised mice bearing human multiple myeloma (H929 and AMO1) xenografts, and its antitumor activity was observed. RESULTS S63845 showed dose-dependent antitumor activity; the maximum tumor growth inhibition (TGImax) was 114% in the AMO1 model and 103% in the H929 model. [1] |
| Molecular Weight | 829.26 |
| Formula | C39H37ClF4N6O6S |
| Cas No. | 1799633-27-4 |
| Smiles | CN1CCN(CCOc2ccc(-c3c(sc4ncnc(O[C@@H](Cc5ccccc5OCc5ccnn5CC(F)(F)F)C(O)=O)c34)-c3ccc(F)o3)c(C)c2Cl)CC1 |
| Relative Density. | 1.46 g/cm3 (Predicted) |
| Storage | store at low temperature,keep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 33.33 mg/mL (40.19 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.41 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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