RG7112 - CAS:939981-39-2

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RG7112 (Synonyms:RO5045337)

目录号 : KM4974 CAS No. : 939981-39-2 纯度 : 98%

Data Sheet 产品使用指南

RG7112 是有效的、选择性的、第一个用于临床的、可口服的、可透过血脑屏障的、 MDM2-p53 抑制剂，IC₅₀ 值为 18 nM，结合到MDM2 的K_D 值为 11 nM.

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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 K_D of 11 nM for binding to MDM2.

体外研究

RG7112 (0-5 μM) stabilizes wild-type p53 and induces p53 signaling in cancer cells. RG7112 effectively activates p53 functions in cancer cells.

Cell Proliferation Assay

Cell Line:	SJSA1 osteosarcoma cells.
Concentration:	0-5 μM.
Incubation Time:	0-60 hours.
Result:	Dose-dependently inhibited the growth and killed SJSA1 osteosarcoma cells expressing high levels of MDM2 protein due to MDM2 gene amplification.

Cell Cycle Analysis

Cell Line:	HCT116 and SJSA1 cells.
Concentration:	0-5 μM.
Incubation Time:	48 hours.
Result:	Induced a dose-dependent cell cycle block in G1 and G2/M phase and depletion of the S phase compartment.

体内研究

RG7112 (25-200 mg/kg, single oral dose) activates p53 pathway and induces apoptosis in tumor cells in vivo.
RG7112 (100 mg/kg, gavage once per day, 5 days/week for 3 weeks ) reduces tumor growth rate and increases survival in GBM models.

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.

分子式

C₃₈H₄₈Cl₂N₄O₄S

分子量

727.78

CAS号

939981-39-2

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

溶解性数据

In Vitro:

DMSO : 200 mg/mL (274.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3740 mL	6.8702 mL	13.7404 mL
5 mM	0.2748 mL	1.3740 mL	2.7481 mL
10 mM	0.1374 mL	0.6870 mL	1.3740 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: ≥ 10 mg/mL (13.74 mM); Clear solution

此方案可获得 ≥ 10 mg/mL (13.74 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 100.0 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% corn oil
Solubility: ≥ 10 mg/mL (13.74 mM); Clear solution

此方案可获得 ≥ 10 mg/mL (13.74 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 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
3.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 5 mg/mL (6.87 mM); Clear solution
4.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (3.44 mM); Clear solution

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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KKL 顾客使用本产品发表的 9 篇科研文献

The molarity calculator equation

The dilution calculator equation