Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
50mg |
|
||
100mg |
|
||
Other Sizes |
|
ln Vitro |
S65487 attaches itself to BCL-2's BH3 hydrophobic groove. S65487 has IC50s in the low nM range and inhibits cell proliferation by inducing apoptosis in a panel of hematological cancer cell lines[1].
|
---|---|
ln Vivo |
S65487, when administered intravenously (IV), completely suppresses BCL-2-dependent RS4;11 cancers in vivo. Once weekly IV injection of S65487 in conjunction with the MCL-1-specific inhibitor S64315/MIK665 results in well tolerated doses of strong and permanent tumor shrinkage in xenograft models of lymphoid malignancies in mice and rats[1].
|
References |
[1]. Arnaud Le Tiran, et al. Abstract 1276: Identification of S65487/VOB560 as a potent and selective intravenous 2nd-generation BCL-2 inhibitor active in wild-type and clinical mutants resistant to Venetoclax. Cancer Research. July 2021.
[2]. American Association for Cancer Research, AACR. 2021.4.10-15. |
Molecular Formula |
C41H41CLN6O4
|
---|---|
Molecular Weight |
717.26
|
CAS # |
1644600-79-2
|
Related CAS # |
S65487 sulfate;2416937-01-2;S65487 hydrochloride;1644543-95-2
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
N1(C)C(C2=CC(Cl)=CC=C2C(N2[C@H](CN3CCOCC3)CC3=C(C2)C=CC=C3)=O)=CC(C(N(C2C=C(C#N)N(C)C=2C)C2=CC=C(O)C=C2)=O)=C1C
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : 200 mg/mL (278.84 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 50.0 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: ≥ 5 mg/mL (6.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3942 mL | 6.9710 mL | 13.9419 mL | |
5 mM | 0.2788 mL | 1.3942 mL | 2.7884 mL | |
10 mM | 0.1394 mL | 0.6971 mL | 1.3942 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.