Home>>Signaling Pathways>> Proteases>> E1/E2/E3 Enzyme>>RO8994
RO8994 目录号 GC19312

规格 价格 库存 购买数量
5mg
¥1,710.00
现货
10mg
¥2,610.00
现货
50mg
¥9,900.00
现货
100mg
¥17,100.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1309684-94-3 SDF Download SDF
别名 N/A
化学名 N/A
Canonical 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
分子式 C31H31Cl2FN4O4 分子量 613.51
溶解度 DMSO : ≥ 45 mg/mL (73.35 mM) 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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产品描述

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: MDM2in 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:
[1]. Zhang Z, et al. Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg Med Chem. 2014 Aug 1;22(15):4001-4009.