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S65487 (VOB560) is a potent and selective inhibitor of the anti-apoptotic protein Bcl-2, displaying activity not only against the wild-type protein but also against clinically relevant BCL-2 mutations such as G101V and D103Y. S65487 demonstrates poor affinity toward other Bcl-2 family members, including MCL-1, BFL-1, and BCL-XL, which underlines its selectivity profile. S65487 induces apoptosis in cancer cells and exhibits robust anticancer activities in preclinical studies.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $139 | In Stock | |
5 mg | $347 | In Stock | |
10 mg | $579 | In Stock | |
25 mg | $1,160 | In Stock | |
1 mL x 10 mM (in DMSO) | $548 | In Stock |
Description | S65487 (VOB560) is a potent and selective inhibitor of the anti-apoptotic protein Bcl-2, displaying activity not only against the wild-type protein but also against clinically relevant BCL-2 mutations such as G101V and D103Y. S65487 demonstrates poor affinity toward other Bcl-2 family members, including MCL-1, BFL-1, and BCL-XL, which underlines its selectivity profile. S65487 induces apoptosis in cancer cells and exhibits robust anticancer activities in preclinical studies. |
In vitro | S65487 effectively induces apoptosis and inhibits proliferation in a panel of hematologic cancer cell lines by binding to the BH3 hydrophobic groove of the BCL-2 protein, with a half-maximal inhibitory concentration (IC50) in the low nanomolar (nM) range. [1] |
In vivo | S65487 effectively induces complete regression in BCL-2-dependent RS4;11 tumors through a single intravenous (IV) dose and demonstrates consistent, strong tumor regression in mouse and rat xenograft models of lymphoid malignancies at tolerable doses with weekly IV administrations when combined with MCL-1-specific inhibitor S64315/MIK665.[1] |
Synonyms | VOB560, VOB 560 |
Molecular Weight | 717.26 |
Formula | C41H41ClN6O4 |
Cas No. | 1644600-79-2 |
Smiles | N(C(=O)C=1C=C(N(C)C1C)C2=C(C(=O)N3[C@H](CN4CCOCC4)CC=5C(C3)=CC=CC5)C=CC(Cl)=C2)(C=6C=C(C#N)N(C)C6C)C7=CC=C(O)C=C7 |
Color | Yellow |
Appearance | Solid |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 160 mg/mL (223.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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