Rintodestrant (G1T48) 是具有口服活性的、非甾体类的、选择性的雌激素受体 (estrogen receptor) 的降解剂。Rintodestrant (G1T48) 也是CDK4/6的抑制剂。
生物活性 | Rintodestrant (G1T48) is an orally active, non-steroidal and selectiveestrogen receptordegrader. Rintodestrant (G1T48) is also aCDK4/6inhibitor[1]. |
体外研究 (In Vitro) | Rintodestrant (G1T48) is a potent and efficacious inhibitor of estrogen-mediated transcription and proliferation in ER-positive breast cancer cells, similar to the pure antiestrogen fulvestrant[1]. Rintodestrant (G1T48) selectively inhibits the growth of ER-positive, but not ER-negative, breast cancer cells[1].
Cell Viability Assay[1] Cell Line: | MCF7 cells. | Concentration: | 1 pM-1 μM. | Incubation Time: | 18 h. | Result: | Downregulates the estrogen receptor in breast cancer cells. Significantly inhibited estrogen-mediated growth of MCF7 cells demonstrating approximately threefold higher potency when compared to Fulvestrant. Does not impact apoptosis in MCF7 breast cancer cells.
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体内研究 (In Vivo) | Rintodestrant (G1T48, 30 or 100 mg/kg) inhibits estrogen signaling in endocrine-resistant breast cancer models[1].
Animal Model: | MCF7 xenograft tumors[1]. | Dosage: | 30 or 100 mg/kg. | Administration: | P.O. daily for 28 days. | Result: | Demonstrated dose-dependent inhibition of TamR tumor growth. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(108.11 mM;Need ultrasonic) 配制储备液 1 mM | 2.1622 mL | 10.8110 mL | 21.6221 mL | 5 mM | 0.4324 mL | 2.1622 mL | 4.3244 mL | 10 mM | 0.2162 mL | 1.0811 mL | 2.1622 mL |
*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。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 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 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.41 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.41 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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