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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 | Availability | Quantity |
---|---|---|---|
1 mg | $79 | In Stock | |
5 mg | $148 | In Stock | |
10 mg | $247 | In Stock | |
25 mg | $443 | In Stock | |
50 mg | $653 | 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 | MCL1:0.19 nM (Kd) |
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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 33.33 mg/mL (40.19 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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