产品
编 号：F529579
分子式：C38H48Cl2N4O4S
分子量：727.78
分子式：C38H48Cl2N4O4S
分子量：727.78
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 939981-39-2
产品详情
生物活性：
RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.
体内研究：
RG7112 (25 -200 mg/kg，单次口服) 在体内激活p53通路并诱导肿瘤细胞凋亡。 RG7112 (100 mg/kg，每天灌胃一次，5 天/周，持续 3 周) 在 GBM 模型中降低肿瘤生长速度并提高存活率。Animal Model:Female Balb/c nude mice.
Dosage:25-200 mg/kg.
Administration:Orally, single dose.
Result:At the highest dose level of RG7112 (200 mg/kg) only 1.2% (± 0.89 SD) of cells incorporated BrdU at 24 h post-dosing, vs. 14% (± 1.83 SD) of vehicle treated tumors.
Animal Model:GBM cells were implanted into the brain of Athymic Nude mice (7 weeks old females, 10 animals/group).
Dosage:100 mg/kg.
Administration:Oral gavage, once per day, 5 days/week for 3 weeks.
Result:Reduced tumor growth rate and increases survival in heterotopic and orthotopic animal models bearing MDM2-amplified GBM.
体外研究：
RG7112 (0-5 μM) 稳定野生型 p53 并在癌细胞中诱导 p53 信号传导。RG7112 有效激活癌细胞中的 p53 功能。
RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.
体内研究：
RG7112 (25 -200 mg/kg，单次口服) 在体内激活p53通路并诱导肿瘤细胞凋亡。 RG7112 (100 mg/kg，每天灌胃一次，5 天/周，持续 3 周) 在 GBM 模型中降低肿瘤生长速度并提高存活率。Animal Model:Female Balb/c nude mice.
Dosage:25-200 mg/kg.
Administration:Orally, single dose.
Result:At the highest dose level of RG7112 (200 mg/kg) only 1.2% (± 0.89 SD) of cells incorporated BrdU at 24 h post-dosing, vs. 14% (± 1.83 SD) of vehicle treated tumors.
Animal Model:GBM cells were implanted into the brain of Athymic Nude mice (7 weeks old females, 10 animals/group).
Dosage:100 mg/kg.
Administration:Oral gavage, once per day, 5 days/week for 3 weeks.
Result:Reduced tumor growth rate and increases survival in heterotopic and orthotopic animal models bearing MDM2-amplified GBM.
体外研究：
RG7112 (0-5 μM) 稳定野生型 p53 并在癌细胞中诱导 p53 信号传导。RG7112 有效激活癌细胞中的 p53 功能。
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