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A-385358 is a selective Bcl-xL inhibitor with Kis of 0.80 nM for Bcl-xL and 67 nM for Bcl-2, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 52 € | In Stock | |
5 mg | 111 € | In Stock | |
10 mg | 168 € | In Stock | |
25 mg | 282 € | In Stock | |
50 mg | 422 € | In Stock | |
100 mg | 598 € | In Stock | |
1 mL x 10 mM (in DMSO) | 160 € | In Stock |
Description | A-385358 is a selective Bcl-xL inhibitor with Kis of 0.80 nM for Bcl-xL and 67 nM for Bcl-2, respectively. |
Targets&IC50 | BCL-XL:0.8 nM (ki), BCL2:67 nM (ki) |
In vitro | In IL-3-deprived FL5.12/Bcl-XL cells, A-385358 results in cell killing with an EC50 of 0.47 μM and increases caspase-3 activity. The EC50 of A-385358 for IL-3-depleted FL5.12/Bcl-2 cells with an EC50 of 1.9 μM which is 4-fold higher relative to the cytokine-deprived FL5.12/Bcl-XL cells. A-385358 stimulates more cytochrome c release from mitochondria isolated from FL5.12/Bcl-XL versus Bcl-2 cells[1]. |
In vivo | The combination of A-385358 (75 mg/kg) plus paclitaxel (30 mg/kg) is well tolerated and inhibits tumor growth rate by nearly 80%. A-385358 exhibits slow but steady increase in the tumor growth. The combination of A-385358 (100 mg/kg) and a lower dose of paclitaxel produces a significant reduction in tumor growth and yields a >100% increase in time for tumors to reach 900 mm3 (%ILS)[1]. |
Molecular Weight | 639.83 |
Formula | C32H41N5O5S2 |
Cas No. | 406228-55-5 |
Smiles | CN(C)CC[C@H](CSc1ccccc1)Nc1ccc(cc1[N+]([O-])=O)S(=O)(=O)NC(=O)c1ccc(cc1)N1CCC(C)(C)CC1 |
Relative Density. | 1.31 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (70.33 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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