RapaLink-1|cas:1887095-82-0|西域试剂

RapaLink-1,98.46%

产品编号：Bellancom-111373| CAS NO：1887095-82-0| 分子式：C₉₁H₁₃₈N₁₂O₂₄| 分子量：1784.14

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-111373	￥4900.00	杭州北京（现货）
Bellancom-111373	￥7000.00	杭州北京（现货）
Bellancom-111373	￥12500.00	杭州北京（现货）
Bellancom-111373	￥20000.00	杭州北京（现货）

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RapaLink-1

产品介绍

RapaLink-1 是第三代 mTOR 抑制剂，通过 linker 将雷帕霉素 (Rapamycin, HY-10219) 与二代 mTOR 抑制剂 MLN0128 (HY-13328) 结合。RapaLink-1 比雷帕霉素或 mTOR 抑制剂 (TORKi) 更有效，能有效地阻断癌源性的，激活的 mTOR 突变体。RapaLink-1 可以穿过血脑屏障。RapaLink-1 与 FKBP12 的结合导致持久抑制 mTORC1。RapaLink-1 通过促进自噬在抗磷脂综合征中发挥抗血栓作用。具有抗癌活性。

生物活性

RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity.

体外研究

RapaLink-1 (0-200 nM; 3 days) shows U87MG cells growth inhibition.
RapaLink-1 (0-12.5 nM; 48 hours) arrests U87MG cells at G0/G1.
RapaLink-1 selectively inhibits p-RPS6^S235/236 and p-4EBP1^T37/46 at doses as low as 1.56 nM.
Rapalink-1 (100 nM; 24 to 96 hours) suppressed renal cell carcinoma (RCC) cell proliferation by inducing apoptosis and cell cycle arrest.
RapaLink-1 exploits the unique juxtaposition of two drug-binding pockets to create a bivalent interaction. RapaLink-1 overcomes resistance to existing first- and second-generation inhibitors.

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

Cell Proliferation Assay

Cell Line:	U87MG cells
Concentration:	0-200 nM
Incubation Time:	3 days
Result:	Showed growth inhibition.

Cell Cycle Analysis

Cell Line:	U87MG cells
Concentration:	0-12.5 nM
Incubation Time:	48 hours
Result:	Arrested cells at G0/G1.

Western Blot Analysis

Cell Line:	U87MG cells
Concentration:	0.39-12.5 nM
Incubation Time:	3 hours
Result:	Selectively inhibited p-RPS6^S235/236 and p-4EBP1^T37/46 at doses as low as 1.56 nM. The mTORC2 targets p-AKT^S473, p-SGK1^S78, and p-NDRG1^T346, and the p-AKT^S473 target p-GSK3β^S9 was inhibited only at high doses.

体内研究
(In Vivo)

RapaLink-1 (i.p.; every 5 days for 25 days, then once a week for 11 week) shows potent anti-tumor efficacy.

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

Animal Model:	BALB/ Cnu/nu mice bearing U87MG intracranial xenografts
Dosage:	1.5 mg/kg
Administration:	I.p.; every 5 days for 25 days, then once a week for 11 week
Result:	Led to initial regression and subsequent stabilization of tumor size.

体内研究

RapaLink-1 (i.p.; every 5 days for 25 days, then once a week for 11 week) shows potent anti-tumor efficacy.

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

Animal Model:	BALB/ Cnu/nu mice bearing U87MG intracranial xenografts
Dosage:	1.5 mg/kg
Administration:	I.p.; every 5 days for 25 days, then once a week for 11 week
Result:	Led to initial regression and subsequent stabilization of tumor size.

体内研究

RapaLink-1 (i.p.; every 5 days for 25 days, then once a week for 11 week) shows potent anti-tumor efficacy.

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

Animal Model:	BALB/ Cnu/nu mice bearing U87MG intracranial xenografts
Dosage:	1.5 mg/kg
Administration:	I.p.; every 5 days for 25 days, then once a week for 11 week
Result:	Led to initial regression and subsequent stabilization of tumor size.

性状

Solid

溶解性数据

In Vitro:

DMSO : 178 mg/mL (99.77 mM; Need ultrasonic and warming)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.5605 mL	2.8025 mL	5.6049 mL
5 mM	0.1121 mL	0.5605 mL	1.1210 mL
10 mM	0.0560 mL	0.2802 mL	0.5605 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 (sealed storage, away from moisture)。-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 90% corn oil
Solubility: ≥ 5 mg/mL (2.80 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (2.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。