RRx-001 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RRx-001 纯度: 99.71%

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。

RRx-001 Chemical Structure

CAS No. : 925206-65-1

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1210	In-stock
5 mg	￥1100	In-stock
10 mg	￥1900	In-stock
50 mg	￥7500	In-stock
100 mg	￥13000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

RRx-001 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Anti-Infection Compound Library
Apoptosis Compound Library
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
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Drug Repurposing Compound Library
Anti-COVID-19 Compound Library
Anti-Lung Cancer Compound Library
Anti-Blood Cancer Compound Library
Antiparasitic Compound library
Rare Diseases Drug Library

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^[1]. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α^[2]. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity^[3].

体外研究
(In Vitro)

RRx-001 (0-5 μM, 24 hours) inhibits MM cells growth and overcomes resistance to novel and conventional therapies^[1].
RRx-001 blocks migration of MM cells and associated angiogenesis^[1].
RRx-001 induces significant G1 phase growth arrest, with concomitant decrease in S phase. RRx-001 triggers significant apoptosis in MM cells^[1].
RRx-001 inhibits DNA methylation by downregulating DNA methytransferases^[1].
RRx-001 and the supernatant of RRx-001-treated macrophages downregulates CD47 on tumor cells and SIRPα on macrophages^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

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
(In Vivo)

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^[1].
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^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CB-17 SCID-mice were subcutaneously inoculated with 5.0 × 10⁶ MM.1S cells in 100 µL of serum-free RPMI 1640 medium^[1].
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^[2].
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.

Clinical Trial

分子量

268.02

Formula

C₅H₆BrN₃O₅

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。

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 (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。

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
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。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Das DS, et al. A novel hypoxia-selective epigenetic agent RRx-001 triggers apoptosis and overcomes drug resistance in multiple myeloma cells. Leukemia. 2016 Nov;30(11):2187-2197.

[2]. Yalcin O, et al. From METS to malaria: RRx-001, a multi-faceted anticancer agent with activity in cerebral malaria. Malar J. 2015 May 28;14:218.

[3]. Cabrales P, et al. RRx-001 Acts as a Dual Small Molecule Checkpoint Inhibitor by Downregulating CD47 on Cancer Cells and SIRP-α on Monocytes/Macrophages. Transl Oncol. 2019 Apr;12(4):626-632.

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