RRx-001 - CAS:925206-65-1

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RRx-001

目录号 : KM9952 CAS No. : 925206-65-1 纯度 : 98%

Data Sheet 产品使用指南

RRx-001 是一种低氧选择性的表观遗传因子，被用作放射或化疗敏感剂，能诱发凋亡，克服骨髓瘤的耐药性。RRx-001 具有有效的抗癌活性且毒性极低。RRx-001是一个免疫检查点的抑制剂，可下调 CD47 和SIRP-α。RRx-001是G6PD的有效抑制剂，具有较强的抗疟活性。

规格	价格	是否有货
5mg		In-stock
10mg		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

RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.

体外研究

RRx-001 (0-5 μM, 24 hours) inhibits MM cells growth and overcomes resistance to novel and conventional therapies.
RRx-001 blocks migration of MM cells and associated angiogenesis.
RRx-001 induces significant G1 phase growth arrest, with concomitant decrease in S phase. RRx-001 triggers significant apoptosis in MM cells.
RRx-001 inhibits DNA methylation by downregulating DNA methytransferases.
RRx-001 and the supernatant of RRx-001-treated macrophages downregulates CD47 on tumor cells and SIRPα on macrophages.

Cell Viability Assay

Cell Line:	Human MM-cell lines (MM.1S, RPMI-8226, H929, ARP1, KMS-11, OPM2, LR5, ANBL6.WT), along with drug resistant cell lines such as (MM.1R, Dox40, LR5, ANBL6.BR, RPMI-8226).
Concentration:	0-5 μM.
Incubation Time:	24 hours.
Result:	Induced a dose-dependent significant (p < 0.05) decrease in viability of all cell lines.

体内研究

RRx-001 (5 mg/kg or 10 mg/kg, I.V., thrice-weekly for 24 days) inhibits tumor growth and prolongs survival in a xenograft mouse model.
RRx-001 (10 mg/kg, IP, twice a week and once a day) exhibits potent anti-cancer activity on the A549 lung cancer model dependent on the presence of tumor-associated macrophages (TAMs) in tumor tissue.

Animal Model:	CB-17 SCID-mice were subcutaneously inoculated with 5.0 × 10 MM.1S cells in 100 µL of serum-free RPMI 1640 medium.
Dosage:	5 mg/kg or 10 mg/kg.
Administration:	I.V., thrice-weekly for 24 days.
Result:	Blocked MM tumor growth and enhances survival. Treatment was well tolerated, suggested by no apparent weight loss.

Animal Model:	Female BALB/c nude mice (19.2 ± 1.7 g) based on A549 lung cancer model.
Dosage:	10 mg/kg.
Administration:	IP, twice a week and once a day.
Result:	Resulted in the most significant tumor growth retardation. Reduction of resident macrophages in tumor-bearing mice attenuates the antitumor activity of RRx-001.

分子式

C₅H₆BrN₃O₅

分子量

268.02

CAS号

925206-65-1

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 : ≥ 100 mg/mL (373.11 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7311 mL	18.6553 mL	37.3107 mL
5 mM	0.7462 mL	3.7311 mL	7.4621 mL
10 mM	0.3731 mL	1.8655 mL	3.7311 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 (9.33 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.33 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-CD in saline)
Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.33 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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.33 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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*

重置计算

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 3 篇科研文献

The molarity calculator equation

The dilution calculator equation