S65487 hydrochloride (Synonyms: VOB560 hydrochloride) |
カタログ番号GC63426
One-Click Copy Product Info
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S65487 (VOB560) 塩酸塩は、強力で選択的な Bcl-2 阻害剤であり、S55746 のプロドラッグです。 S65487 塩酸塩は、G101V や D103Y などの BCL-2 変異に対しても活性があります。 S65487 塩酸塩は、MCL-1、BFL-1、BCL-XL との親和性が低くなります。 S65487塩酸塩はアポトーシスを誘導し、抗がん作用を持っています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1644543-95-2
Sample solution is provided at 25 µL, 10mM.
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S65487 (VOB560) hydrochloride is a potent and selective Bcl-2 inhibitor. S65487 hydrochloride is also active on BCL-2 mutations, such as G101V and D103Y. S65487 hydrochloride has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 hydrochloride induces apoptosis and has anticaner activities[1][2].
S65487 hydrochloride binds to the BH3 hydrophobic groove of BCL-2. S65487 hydrochloride induces apoptosis in a panel of hematological cancer cell lines and inhibits cell proliferation with IC50s in the low nM range[1].
S65487 hydrochloride induces complete regression in BCL-2-dependent RS4;11 tumors in vivo after a single IV (intravenous) administration. Strong and persistent tumor regression in xenograft models of lymphoid malignancies in mouse and rat are observed at well tolerated doses following weekly IV administration of S65487 hydrochloride in combination with the MCL-1-specific inhibitor, S64315/MIK665[1].
[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.
| Cas No. | 1644543-95-2 | SDF | |
| 同義語 | VOB560 hydrochloride | ||
| Formula | C41H42Cl2N6O4 | M.Wt | 753.72 |
| 溶解度 | DMSO : 90 mg/mL (119.41 mM; Need ultrasonic) | Storage | 4°C, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.3268 mL | 6.6338 mL | 13.2675 mL |
| 5 mM | 265.4 μL | 1.3268 mL | 2.6535 mL |
| 10 mM | 132.7 μL | 663.4 μL | 1.3268 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)