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Indibulin

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Chemical Structure| 204205-90-3 同义名 : -
CAS号 : 204205-90-3
货号 : A767569
分子式 : C22H16ClN3O2
纯度 : 98%
分子量 : 389.834
MDL号 : MFCD05861105
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(128.26 mM)，配合低频超声助溶，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 Microtubules are dynamic polymers involved in a multitude of cellular processes. Indibulin is a small-molecule microtubule inhibitor that exhibits antitumor activity but does not cause neurotoxicity. Indibulin dose-dependently inhibited the polymerization of purified calf brain tubulin with an IC50 value of ~0.25μM and a maximal inhibition of 90%. [1] Indibulin inhibited the proliferation of MCF-7 cells with an IC50 value of 150 ± 13nM. Cells treated with 600nM indibulin showed an increased percentage of phosphohistone H3 (S10) compared to the control group. The disruption of the microtubule network was observed when MCF-7 cells were treated with 300nM indibulin. In cells incubated with 600nM indibulin, most of the microtubules were depolymerized compared to the control group. The rates of growth and shortening states of microtubules in MCF-7 cells were reduced by 37 and 53%, respectively, in the presence of 150nM indibulin. Treatment of MCF-7 cells with indibulin (300 and 600nM) increased the levels of Mad2 and BubR1 and activated apoptotic cell death. The combination of indibulin (50 and 150nM) and 1nM vinblastine inhibited the proliferation of MCF-7 cells by 53 and 71%, respectively.[2] In a rat Yoshida AH13 sarcoma model, administration of indibulin (10mg/kg, p.o.) for two weeks resulted in complete tumor remissions.[3]
作用机制 Indibulin is a synthetic inhibitor of tubulin assembly that inhibits microtubule dynamics by blocking mitosis.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.83mL

2.57mL

1.28mL

25.65mL

5.13mL

2.57mL
参考文献

[1]Wienecke A, Bacher G. Indibulin, a novel microtubule inhibitor, discriminates between mature neuronal and nonneuronal tubulin. Cancer Res. 2009;69(1):171-177. doi:10.1158/0008-5472.CAN-08-1342

[2]Kapoor S, Srivastava S, Panda D. Indibulin dampens microtubule dynamics and produces synergistic antiproliferative effect with vinblastine in MCF-7 cells: Implications in cancer chemotherapy. Sci Rep. 2018;8(1):12363. Published 2018 Aug 17. doi:10.1038/s41598-018-30376-y

[3]Bacher G, Nickel B, Emig P, et al. D-24851, a novel synthetic microtubule inhibitor, exerts curative antitumoral activity in vivo, shows efficacy toward multidrug-resistant tumor cells, and lacks neurotoxicity. Cancer Res. 2001;61(1):392-399.