[CAS NO. 1309684-94-3] RO8994
PRODUCTS SPECIFICATIONS [1309684-94-3]
DESCRIPTION [1309684-94-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 613.51 |
| Molecular Formula | C31H31Cl2FN4O4 |
| SMILES | O=C([C@H](N[C@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@@]31C(NC4=C3C=CC(Cl)=C4)=O)NC5=CC=C(C(N)=O)C=C5OC |
Summary
RO8994 is a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitor , with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). IC50 value: 5 nM (in HTRF binding assays), 20 nM (in MTT proliferation assays) Target: MDM2 in vitro: RO8994 represents a new generation of p53-MDM2 antagonists with marked improvement in pharmacological properties for potential clinical development. RO8994 induces dose-dependent up-regulation of p53 target genes and apoptosis in wild-type p53 cancer cells, consistent with its non-genotoxic mechanism of p53 activation. in vivo: RO8994 displays remarkable tumor growth inhibition in the wild-type p53, MDM2-amplified SJSA-1 osteosarcoma tumor xenograft model - exhibiting significant (>60%) tumor growth inhibition at the low dose of 1.56 mg/kg, tumor stasis at 3.125 mg/kg and regression at 6.25 mg/kg.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 45 mg/mL ( 73.35 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6300 mL | 8.1498 mL | 16.2997 mL |
| 5 mM | 0.3260 mL | 1.6300 mL | 3.2599 mL |
| 10 mM | 0.1630 mL | 0.8150 mL | 1.6300 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.39 mM); Clear solution