2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. RGN6024

RGN6024 是一种可透过血脑屏障的、具有口服活性且可逆的小分子微管蛋白 (tubulin) 去稳定剂。RGN6024 在生化和细胞实验中均能抑制微管聚合，与 β-微管蛋白的秋水仙碱结合口袋结合 (SPR: Kd = 6.7 μM；tryptophan assay: Kd = 7.4 μM)，并在胶质母细胞瘤 (GB) 细胞中触发 G2/M 期阻滞。RGN6024 在 βIII-微管蛋白过表达的细胞中仍保持活性。RGN6024 在胶质母细胞瘤 (GB) 异种移植小鼠模型中可抑制肿瘤生长。RGN6024 可用于胶质母细胞瘤 (GB) 的研究。

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RGN6024

RGN6024 Chemical Structure

CAS No. : 3055038-20-2

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RGN6024 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB)[1].

体外研究
(In Vitro)

RGN6024 (100 nM, 48 h) 与 β-微管蛋白的秋水仙碱结合位点结合，并破坏 U87 胶质母细胞瘤细胞中的微管形态[1]。
RGN6024 (72 h) 可逆地降低胶质母细胞瘤细胞的活力，在 U87 细胞中的 IC50 为 85 nM，在 LN-18 细胞中为 23 nM，在 BT142 细胞中为 120 nM[1]。
RGN6024 (0.001-100 μM, 6 h) 在 U87 细胞活力洗脱实验中显示出高可逆性，洗脱后 IC50 为 2482 nM (与未洗脱时的 81.6 nM 相比有 30 倍的变化)[1]。
RGN6024 (250 nM, 48 h) 诱导 U87 细胞发生 G2/M 期阻滞，且在 HeLa 细胞中不易受 βIII-微管蛋白过表达的影响[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RGN6024 相关抗体:

Immunofluorescence[1]

Cell Line: U87 glioblastoma cells
Concentration: 100 nM
Incubation Time: 48 h
Result: Showed loss of MT bundles and changes in cell shape relative to DMSO-treated cells.

Cell Cycle Analysis[1]

Cell Line: U87 glioblastoma cells
Concentration: 250 nM
Incubation Time: 48 h
Result: Induced G2/M arrest in U87 cells.
体内研究
(In Vivo)

RGN6024 (7.5-25 mg/kg，口服，每日一次或 5 天给药/2 天停药，15 天) 在 Temozolomide (TMZ) (HY-17364) 耐药的胶质母细胞瘤异种移植小鼠模型中可抑制肿瘤生长[1]。
RGN6024 (15-20 mg/kg，口服，每日一次或两次，或每两天一次，49 天) 在原位胶质母细胞瘤异种移植小鼠模型中可抑制肿瘤生长并延长生存期[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: LN-18 cells (10×106) in 0.2 mL PBS/Matrigel (50:50) were injected subcutaneously into the upper right flank of female CB17 SCID mice aged 6-8 weeks[1]
Dosage: 7.5, 15 mg/kg daily or 25 mg/kg 5days-on/2days-off (combined with Temozolomide)
Administration: p.o. daily or 5days-on/2days-off (combined with Temozolomide) for 49 days
Result: Reduced tumor growth by 72% and 60% at doses of 7.5 and 15 mg/kg, respectively.
Animal Model: BT142 mut/cells (IDH1 R132H) engineered to express luciferase (BT142-Luc) were stereotactically inoculated into the caudate nucleus of the right brain hemisphere of 6-8-week-old anesthetized BALB/c nude female mice[1]
Dosage: 15 mg/kg once daily 15 mg/kg twice daily, 20 mg/kg once daily and 20 mg/kg on alternate days
Administration: p.o. for 49 days
Result: Showed a statistically significant decrease in tumor size treated with 15 mg/kg twice daily and 20 mg/kg once daily.
Showed no significant change in the body weight.
Improved survival relative to control animals.
分子量

403.46

Formula

C18H21N5O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

RGN6024 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RGN60243055038-20-2RGN 6024RGN-6024Microtubule/TubulinglioblastomatubulinU87 cellsLN-18 cellsInhibitorinhibitorinhibit

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