D-64131

产品说明书

Print
Chemical Structure| 74588-78-6 同义名 : -
CAS号 : 74588-78-6
货号 : A847326
分子式 : C16H13NO2
纯度 : 99%+
分子量 : 251.28
MDL号 : MFCD04039791
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(417.86 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
动物实验配方：
生物活性
描述 Tubulin, the subunit protein of microtubules, is an alpha/beta heterodimer. In many organisms, both alpha and beta exist in numerous isotypic forms encoded by different genes. In addition, both alpha and beta undergo a variety of posttranslational covalent modifications, including acetylation, phosphorylation, detyrosylation, polyglutamylation, and polyglycylation[3]. Tubulins play crucial roles in cell division, intracellular traffic, and cell shape. Tubulin concentration is autoregulated by feedback control of messenger RNA (mRNA) degradation via an unknown mechanism[4]. D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM[5]. The proliferation of tumor cells from 12 of 14 different organs and tissues was inhibited with mean IC(50)s of 62 nM and 24 nM by D-64131 and D-68144, respectively, comparable with the potency of paclitaxel with mean IC(50) of 10 nM. In animal studies, no signs of systemic toxicity were observed after p.o. dosages of up to 400 mg/kg of D-64131. In xenograft experiments with the human amelanoic melanoma MEXF 989, D-64131 was highly active with treatment resulting in a growth delay of 23.4 days at 400 mg/kg[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.98mL

0.80mL

0.40mL

19.90mL

3.98mL

1.99mL

39.80mL

7.96mL

3.98mL
参考文献

[1]Beckers T, Reissmann T, et al. 2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors. Cancer Res. 2002 Jun 1;62(11):3113-9.

[2]Mahboobi S, Pongratz H, et al. Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents. J Med Chem. 2001 Dec 20;44(26):4535-53.

[3]R F Ludueña. Multiple forms of tubulin: different gene products and covalent modifications. Int Rev Cytol.1998;178:207-75.

[4]Zhewang Lin,et al. TTC5 mediates autoregulation of tubulin via mRNA degradation. Science. 2020 Jan 3;367(6473):100-104.

[5]Benny Bang-Andersen. Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 2011 May 12;54(9):3206-21.

[6]Thomas Beckers,et al. 2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors. Cancer Res. 2002 Jun 1;62(11):3113-9.