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CAS No.: 361185-42-4

RBC8 Catalog No. CSN17256

Synonyms: N/A

RBC8 is an inhibitor of GTPases RalA and RalB with IC50 of 3.5 μM in cell assay.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The Ras-like GTPases RalA and RalB are important drivers of the proliferation, survival and metastasis of human cancers. RBC8 inhibits the activation of Ras-like GTPases by blocking the binding of RalA or RalB to its effector Ral Binding Protein 1 (RalBP1). The IC₅₀ values for RBC8 are 3.5μM in H2122 lung cancer cells and 3.4μM in H358 lung cancer cells. When RalA and B were knocked down in H2122 and H358 cells by siRNA, RBC8 treatment showed no further inhibition of colony formation. In addition, RBC8 at 2-16 µM inhibited the spreading of WT murine embryonic fibroblasts (MEFs) but not Cav1^-/- MEFs. In mice bearing H2122 xenograft tumors, intraperitoneal injection of RBC8 (50 mg/kg/d) for 21 days inhibited tumor growth to a similar level as the knockdown of both RalA and RalB. The same treatment of RBC8 on mice inoculated with H358 cancer cells yielded similar results. Moreover, treating H2122 xenograft tumors (median size 250 mm³) with a single intraperitoneal injection of 50mg/kg RBC8 significantly inhibited the activation of both RalA and RalB^[2].

动物研究

剂量

Mice: 10 mg/kg - 50 mg/kg^[1] (i.p.)

给药途径

i.p.

动物药代数据

Animal	Nude mice^[1]
Dose	50 mg/kg
Administration	i.p.
C_max	41.2 ± 4.2 μM
T_1/2	0.58 ± 0.26 h
AUC_{0→5 h}	139.6 ± 18.8 μg·h/ml

参考文献

[1] Yan C, Liu D, et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-7.
[2] Yan C, Liu D, Li L, Wempe MF, Guin S, Khanna M, Meier J, Hoffman B, Owens C, Wysoczynski CL, Nitz MD, Knabe WE, Ahmed M, Brautigan DL, Paschal BM, Schwartz MA, Jones DN, Ross D, Meroueh SO, Theodorescu D. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-7. doi: 10.1038/nature13713. Epub 2014 Sep 14. PMID: 25219851; PMCID: PMC4351747.

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
- 2.3560 mL
- 11.7799 mL
- 23.5598 mL
- 5 mM
- 0.4712 mL
- 2.3560 mL
- 4.7120 mL
- 10 mM
- 0.2356 mL
- 1.1780 mL
- 2.3560 mL

技术信息

CAS号

361185-42-4

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H20N4O3

运输

蓝冰

分子量

424.45

别名

N/A

溶解度

DMSO	50.0 mg/mL (117.8 mM)
Water	insoluble

动物实验配方

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RBC8 Catalog No. CSN17256

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