Rintodestrant G1T48|cas:2088518-51-6|西域试剂

Rintodestrant G1T48,99.79%

产品编号：Bellancom-137449| CAS NO：2088518-51-6| 分子式：C₂₆H₁₉FO₅S| 分子量：462.49

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-137449		￥5000.00	杭州北京（现货）
Bellancom-137449		￥8500.00	杭州北京（现货）

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Rintodestrant G1T48

产品介绍

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 selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor.

体外研究

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.
Rintodestrant (G1T48) selectively inhibits the growth of ER-positive, but not ER-negative, breast cancer cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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.

体内研究
(In Vivo)

Rintodestrant (G1T48, 30 or 100 mg/kg) inhibits estrogen signaling in endocrine-resistant breast cancer models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MCF7 xenograft tumors.
Dosage:	30 or 100 mg/kg.
Administration:	P.O. daily for 28 days.
Result:	Demonstrated dose-dependent inhibition of TamR tumor growth.

体内研究

Rintodestrant (G1T48, 30 or 100 mg/kg) inhibits estrogen signaling in endocrine-resistant breast cancer models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MCF7 xenograft tumors.
Dosage:	30 or 100 mg/kg.
Administration:	P.O. daily for 28 days.
Result:	Demonstrated dose-dependent inhibition of TamR tumor growth.

体内研究

Rintodestrant (G1T48, 30 or 100 mg/kg) inhibits estrogen signaling in endocrine-resistant breast cancer models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MCF7 xenograft tumors.
Dosage:	30 or 100 mg/kg.
Administration:	P.O. daily for 28 days.
Result:	Demonstrated dose-dependent inhibition of TamR tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (108.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明