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Idasanutlin (Synonyms: RG7388) 纯度: 99.90%
Idasanutlin (RG7388) 是一种有效,选择性的 MDM2 拮抗剂,能够抑制 p53-MDM2 的结合,IC50 值为 6 nM。
Idasanutlin Chemical Structure
CAS No. : 1229705-06-9
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1492 | In-stock | |
2 mg | ¥750 | In-stock | |
5 mg | ¥1100 | In-stock | |
10 mg | ¥1500 | In-stock | |
50 mg | ¥4500 | In-stock | |
100 mg | ¥7200 | In-stock | |
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生物活性 |
Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM. |
IC50 & Target |
IC50: 6 nM (p53-MDM2)[1] |
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体外研究 (In Vitro) |
Idasanutlin (RG7388) inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53[1]. Idasanutlin (RG7388) (300 nM or 1.8 μM) induces apoptosis in SJSA osteosarcoma cells[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Idasanutlin (RG7388, 25 mg/kg p.o.) results in tumor growth inhibition and regression, in the mouse SJSA human osteosarcoma xenograft model[1]. Idasanutlin (RG7388) induces induction of apoptosis and antiproliferation, in the SJSA xenograft model[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
616.48 |
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Formula |
C31H29Cl2F2N3O4 |
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CAS 号 |
1229705-06-9 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 45 mg/mL (73.00 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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参考文献 |
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Cell Assay [1] |
Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2] |
At 10 to 12 weeks of age, mice are implanted with a 1:1 mixture of human SJSA osteosarcoma cells (ATCC) suspended in phenol-free Matrigel and PBS. Mice are implanted in the right flank at a concentration of 5×106 cells in 0.2 mL total volume. At approximately day 10, animals are randomized according to tumor volume, so that all groups of 10 randomized mice have similar starting mean tumor volumes of 100 to 250 mm3. Idasanutlin (RG7388) is administered as an amorphous solid dispersion microbulk precipitate powder containing 30% drug substance and 70% hydroxypropyl methylcellulose acetate succinate polymer that is reconstituted immediately before administration as a suspension in Klucel/Tween, and remaining suspension is discarded after dosing. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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