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Kevetrin HCl

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Chemical Structure| 66592-89-0 同义名 : 3-氰基丙基异硫脲盐酸盐 ;4-Isothioureidobutyronitrile hydrochloride;thioureidobutyronitrile hydrochloride;NSC 525990;4-Isothioureidobutyronitrile;Kevetrin (hydrochloride);Thioureidobutyronitrile HCl;Kevetrin hydrochloride
CAS号 : 66592-89-0
货号 : A385793
分子式 : C5H10ClN3S
纯度 : 99%+
分子量 : 179.671
MDL号 : MFCD22572767
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(222.63 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(556.57 mM)，配合低频超声助溶
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.57mL

1.11mL

0.56mL

27.83mL

5.57mL

2.78mL

55.66mL

11.13mL

5.57mL
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