RITA (NSC 652287)
(Synonyms: 5,5'-(2,5-呋喃二基)二-2-噻吩甲醇,NSC 652287) 目录号 : GC12793
An inhibitor of the p53-HDM-2 interaction
Cas No.:213261-59-7
Sample solution is provided at 25 µL, 10mM.
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IC50: 2 nM and 20 nM for A-498 and TK-10, respectively
A series of naturally occurring and synthetic compounds containing one or more thiophene moieties have been tested in the NCI Anticancer Drug Screen and have demonstrated differential antiproliferative activity. Thiophene derivatives as a class exhibit very similar patterns of differential sensitivity, the molecular basis for which is not clear. The compound 2,5-bis(5-hydroxymethyl-2-thienyl) furan (NSC 652287), is the most potent thiophene derivative and has been selected as the lead compound for mechanistic studies.
In vitro: A number of cell lines showed a striking differential sensitivity to NSC 652287 when compared with the other cell lines in the panel, with GI50 values of 10–60 nM. The compound was found to decrease the initial number of cells by 50% (LC50) at a concentration of 100 nM in the A-498 cell line, compared with ~100 mM for the majority of the tumor cell lines. The A-498 and TK-10 cell lines were particularly sensitive to NSC 652287-induced cytotoxicity compared with ACHN and UO-31 cell lines [1].
In vivo: NSC 652287 was evaluated against A-498 tumor cell xenografts grown subcutaneously in nude mice. When NSC 652287 was administered twice a day, all three doses resulted in complete tumor regression in 100% of the treated mice by the end of the third treatment period. The tumors did not regrow during the remaining 40 days of the study, and no gross evidence of toxicity was observed. Studies with xenografts derived from other sensitive cell lines including the renal CAKI-1, melanoma UACC-257, ovarian OVCAR-5, and colon HCC-2998, showed moderate or minimal in vivo activity [2].
Clinical trials: Currenlty no clinical data are available.
Reference:
[1] Rivera MI, Stinson SF, Vistica DT, Jorden JL, Kenney S, Sausville EA. Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism. Biochem Pharmacol. 1999;57(11):1283-95.
| Cell experiment [1]: | |
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Cell lines |
Human renal tumor cell lines |
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Preparation method |
The solubility of this compound in DMSO is >14.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
48-hr |
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Applications |
NSC 652287 (48-hr) inhibited cell growth with the GI50 values of 10–60 nM in the tumor cell lines. The A-498 and TK-10 cell lines were particularly sensitive to NSC 652287-induced cytotoxicity with the IC50 values of 2 nM and 20 nM, respectively. |
| Animal experiment [1,2]: | |
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Animal models |
Nude mice bearing A-498 tumor cell xenografts, HCT116 tumor xenografted mouse model |
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Dosage form |
Intravenous injection, 7 hr apart, every 4 days for 12 days |
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Application |
NSC 652287 (44.5 mg/kg, 66.7 mg/kg, 100 mg/kg) resulted in complete tumor regression in 100% of the treated mice by the end of the third treatment period. Intraperitoneal administration of NSC 652287 was well tolerated in mice after, with no observable weight loss at doses up to 10 mg/kg during 1 month. NSC 652287 (0.1 mg/kg, five injections) suppressed the growth of the HCT116 tumors by 40%. NSC 652287 (1 or 10 mg/kg) showed strong antitumor activity. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Rivera M I, Stinson S F, Vistica D T, et al. Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism[J]. Biochemical pharmacology, 1999, 57(11): 1283-1295. [2]. Issaeva N, Bozko P, Enge M, et al. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors[J]. Nature medicine, 2004, 10(12): 1321. | |
| Cas No. | 213261-59-7 | SDF | |
| 别名 | 5,5'-(2,5-呋喃二基)二-2-噻吩甲醇,NSC 652287 | ||
| 化学名 | [5-[5-[5-(hydroxymethyl)thiophen-2-yl]furan-2-yl]thiophen-2-yl]methanol | ||
| Canonical SMILES | C1=C(SC(=C1)C2=CC=C(O2)C3=CC=C(S3)CO)CO | ||
| 分子式 | C14H12O3S2 | 分子量 | 292.4 |
| 溶解度 | ≥ 14.6 mg/mL in DMSO, ≥ 9.84 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.42 mL | 17.0999 mL | 34.1997 mL |
| 5 mM | 0.684 mL | 3.42 mL | 6.8399 mL |
| 10 mM | 0.342 mL | 1.71 mL | 3.42 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet