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CAS No.: 66592-89-0

Kevetrin HCl/盐酸凯维特林 Catalog No. CSN17245

Synonyms: 4-Isothioureidobutyronitrile hydrochloride;thioureidobutyronitrile hydrochloride;4-Isothioureidobutyronitrile HCl

Kevetrin HCl is an activator of the tumor suppressor protein p53 with potential antineoplastic activity.

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技术信息

生物活性

描述Kevetrin Hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity. Kevetrin activates p53 which in turn induces the expressions of p21 and PUMA (p53 up-regulated modulator of apoptosis), thereby inhibiting cancer cell growth and causing tumor cell apoptosis. Kevetrin may be effective in drug-resistant cancers with mutated p53. p53 tumor suppressor, a transcription factor regulating the expression of many stress response genes and mediating various anti-proliferative processes, is often mutated in cancer cells. Moreover, Kevetrin has demonstrated potent anti-tumor efficacy against various carcinoma xenograft models: lung, breast, colon, prostate and squamous cell carcinoma, and in a leukemia tumor model. In drug-resistant cell lines, Kevetrin has shown excellent activity, galvanizing the Company to focus on Kevetrin's development potential in this area. Kevetrin also displayed efficacy against TP53 wild‑type and mutant primary AML (acute myeloid leukemia), with a preferential cytotoxic activity against blast cells^[2].
参考文献

[1] Tripathy D, Harnden K, et al. Next generation sequencing and tumor mutation profiling: are we ready for routine use in the oncology clinic? BMC Med. 2014 Aug 12;12:140.
[2] Napolitano R, De Matteis S, Carloni S, Bruno S, Abbati G, Capelli L, Ghetti M, Bochicchio MT, Liverani C, Mercatali L, Calistri D, Cuneo A, Menon K, Musuraca G, Martinelli G, Simonetti G. Kevetrin induces apoptosis in TP53 wild‑type and mutant acute myeloid leukemia cells. Oncol Rep. 2020 Oct;44(4):1561-1573

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 5.5657 mL
- 27.8286 mL
- 55.6573 mL
- 5 mM
- 1.1131 mL
- 5.5657 mL
- 11.1315 mL
- 10 mM
- 0.5566 mL
- 2.7829 mL
- 5.5657 mL

技术信息

CAS号

66592-89-0

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C5H10ClN3S

运输

蓝冰

分子量

179.67

别名

4-Isothioureidobutyronitrile hydrochloride;thioureidobutyronitrile hydrochloride;4-Isothioureidobutyronitrile HCl;thioureidobutyronitrile HCl;Kevetrin (hydrochloride);4-Isothioureidobutyronitrile;NSC 525990;Kevetrin

溶解度

DMSO	110.0 mg/mL (612.2 mM)
Water	115.0 mg/mL (640.1 mM)

动物实验配方

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Kevetrin HCl/盐酸凯维特林 Catalog No. CSN17245

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