Location : Home > Products > Inhibitors of Meditech > Apoptosis
Name:RO8994
| Chemical structure | Code NO. |
MT0822 |
 |
Name |
RO8994 |
Synonym |
RO 8994; RO-8994 | |
CAS NO. |
1309684-94-3 | |
Chemical Formula |
C31H31Cl2FN4O4 | |
MW |
613.51 | |
Purity |
>98% | |
Solubility(R.T.: 25℃) |
DMSO:45mg/mL | |
Stability |
- 20℃, 2 years |
Availability and price
RO8994 is in stock. Bulk available at low price, welcom to inquire quotation.
We offer big discount for bulk quantities. If you have any other questions or needs, please send email to sales@meditechbs.com. We’ll reply you asap.
Description
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.
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.
References
Attention
Sold for research purposes only; not for human use of any kind.
