S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, is a proagent of S55746. S65487 sulfate is also active on BCL-2 mutations, such as G101V and D103Y. S65487 sulfate has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 sulfate induces apoptosis and has anticaner activities.

Product information

CAS Number: 2416937-01-2

Molecular Weight: 815.33

Formula: C41H43ClN6O8S

Chemical Name: 5-{5-chloro-2-[(3S)-3-[(morpholin-4-yl)methyl]-1,2,3,4-tetrahydroisoquinoline-2-carbonyl]phenyl}-N-(5-cyano-1,2-dimethyl-1H-pyrrol-3-yl)-N-(4-hydroxyphenyl)-1,2-dimethyl-1H-pyrrole-3-carboxamide; sulfuric acid

Smiles: CN1C(=CC(=C1C)N(C1=CC=C(O)C=C1)C(=O)C1C=C(C2C=C(Cl)C=CC=2C(=O)N2CC3=CC=CC=C3C[C@H]2CN2CCOCC2)N(C)C=1C)C#N.OS(O)(=O)=O

InChiKey: ZLAZYXMNPRHARH-WAQYZQTGSA-N

InChi: InChI=1S/C41H41ClN6O4.H2O4S/c1-26-36(41(51)48(31-10-12-34(49)13-11-31)38-21-32(23-43)44(3)27(38)2)22-39(45(26)4)37-20-30(42)9-14-35(37)40(50)47-24-29-8-6-5-7-28(29)19-33(47)25-46-15-17-52-18-16-46;1-5(2,3)4/h5-14,20-22,33,49H,15-19,24-25H2,1-4H3;(H2,1,2,3,4)/t33-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 135 mg/mL (165.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO). H2O : 1.25 mg/mL (1.53 mM; ultrasonic and warming and heat to 60°C).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

S65487 binds to the BH3 hydrophobic groove of BCL-2. S65487 induces apoptosis in a panel of hematological cancer cell lines and inhibits cell proliferation with IC50s in the low nM range.

In Vivo:

S65487 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 in combination with the MCL-1-specific inhibitor, S64315/MIK665.

Products are for research use only. Not for human use.