[CAS NO. 2416937-01-2] S65487sulfate
PRODUCTS SPECIFICATIONS [2416937-01-2]
DESCRIPTION [2416937-01-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 815.33 |
| Molecular Formula | C41H43ClN6O8S |
| SMILES | O=C(C1=C(C)N(C)C(C2=C(C=CC(Cl)=C2)C(N3[C@@H](CC4=CC=CC=C4C3)CN5CCOCC5)=O)=C1)N(C6=CC=C(C=C6)O)C7=C(C)N(C)C(C#N)=C7.O=S(O)(O)=O |
Summary
S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, is a prodrug 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 [1] [2] .
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 IC 50 s in the low nM range [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04702425 | Novartis Pharmaceuticals|Novartis |
Non-Hodgkin Lymphoma (NHL)|Acute Myeloid Leukemia (AML)|Multiple Myeloma (MM)
|
June 23, 2021 | Phase 1 |
| NCT04742101 | Institut de Recherches Internationales Servier|ADIR, a Servier Group company|Servier |
Acute Myeloid Leukemia
|
March 10, 2021 | Phase 1|Phase 2 |
| NCT03755154 | Institut de Recherches Internationales Servier|ADIR, a Servier Group company|Servier |
Relapsed or Refractory Acute Myeloid Leukemia|Relapsed or Refractory Non-Hodgkin Lymphoma|Relapsed or Refractory Multiple Myeloma|Relapsed or Refractory Chronic Lymphocytic Leukemia
|
July 17, 2019 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 135 mg/mL ( 165.58 mM ; Need ultrasonic)
H 2 O : 1.25 mg/mL ( 1.53 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.2265 mL | 6.1325 mL | 12.2650 mL |
| 5 mM | 0.2453 mL | 1.2265 mL | 2.4530 mL |
| 10 mM | 0.1226 mL | 0.6132 mL | 1.2265 mL |