| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| ln Vitro |
In fluorescence polarization tests, A-385358 is a selective inhibitor of Bcl-XL with Kis values of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively. After administering A-385358 to IL-3-deficient FL5.12/Bcl-XL cells for a whole day, the cells died, with an EC50 of 0.47±0.05 μM (n=68). An increase in caspase-3 activity coincides with this impact. The results indicate that Bcl-XL has a stronger affinity than Bcl-2 hydrophobic groove, as evidenced by the 4-fold higher EC50 of A-385358 on IL-3-depleted FL5.12/Bcl-2 cells (1.9±0.1 μM; n=55) in comparison to cytokine-deprived FL5.12/Bcl-XL cells. Additionally, compared to Bcl-2 cells, A-385358 was more successful in inducing the release of cytochrome c from mitochondria isolated from FL5.12/Bcl-XL [1].
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| ln Vivo |
In comparison to paclitaxel monotherapy, the combination of A-385358 at 100 mg/kg/d and a lower dose of paclitaxel significantly reduced tumor growth (%T/C). In addition, compared to vehicle control, the combination more than 100% accelerated the time it took for tumors to reach 900 mm3 (%ILS). When A-385358 was dosed, maximum efficacy was seen, and after therapy was stopped, tumor growth increased gradually but steadily. In addition to being well tolerated, the combination of 30 mg/kg/d paclitaxel and 75 mg/kg/d A-385358 reduced tumor development by over 80%. At dosages as low as 50 mg/kg/d, notable impacts on tumor development were seen in comparison to paclitaxel monotherapy [1].
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| References |
| Molecular Formula |
C32H41N5O5S2
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|---|---|
| Molecular Weight |
639.83
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| Exact Mass |
639.254
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| CAS # |
406228-55-5
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| PubChem CID |
11556440
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| Appearance |
White to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.649
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| LogP |
7.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
44
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1(CCN(CC1)C2=CC=C(C=C2)C(=O)NS(=O)(=O)C3=CC(=C(C=C3)N[C@H](CCN(C)C)CSC4=CC=CC=C4)[N+](=O)[O-])C
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| InChi Key |
DWEHITNKTMMZBR-RUZDIDTESA-N
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| InChi Code |
InChI=1S/C32H41N5O5S2/c1-32(2)17-20-36(21-18-32)26-12-10-24(11-13-26)31(38)34-44(41,42)28-14-15-29(30(22-28)37(39)40)33-25(16-19-35(3)4)23-43-27-8-6-5-7-9-27/h5-15,22,25,33H,16-21,23H2,1-4H3,(H,34,38)/t25-/m1/s1
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| Chemical Name |
N-[4-[[(2R)-4-(Dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-(4,4-dimethylpiperidin-1-yl)benzamide
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| Synonyms |
A 385358 A385358A-385358
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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) |
DMSO : ~50 mg/mL (~78.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.91 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 sonication.
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. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5629 mL | 7.8146 mL | 15.6292 mL | |
| 5 mM | 0.3126 mL | 1.5629 mL | 3.1258 mL | |
| 10 mM | 0.1563 mL | 0.7815 mL | 1.5629 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.
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