|2,2'-[[二氢-2-(4-吡啶基)-1,3(2H,4H)-嘧啶二基]二(亚甲基)]二[N,N-二甲基苯胺]|CsnPharm

CAS No.: 500579-04-4

2,2'-((2-(Pyridin-4-yl)dihydropyrimidine-1,3(2H,4H)-diyl)bis(methylene))bis(N,N-dimethylaniline) Catalog No. CSN15989

Synonyms: NSC 136476

GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, and displays selectivity over other pathways.

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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

靶点 Hedgehog

IC50:5μM
描述The zinc-finger transcription factors Gli1, Gli2, and Gli3 are the prime transcriptional effectors of Hedgehog (Hh) signaling pathway involved in several malignancies, at least one constitutive activation of which is critical importance for cancer development. GANT61 is a downstream inhibitor of Hedgehog signaling (below smo and Sufu) with IC50 value of about 5μM for the inhibition of Hedgehog reporter activity in Shh-L2 cells, which may target on Gli1. A significant decreased expression of Hh target genes, Gli1 and Hip1 on mRNA level can be observed in Sufu^-/- cells treated with 10μM GANT61 for 3 days, while a slight increase of Gli1 could be observed at 2μM. Consistent with the inhibition of Hedgehog signaling, treatment with 5μM GANT 61 for 48h led to a significant reduction of GLI1 and a slight reduction of PTCH expression in both 22Rv1 and PANC1 cells, as well as a cell proliferative inhibition of about 50%. Subcutaneous injection with 50mg/kg GANT 61 for 16 days, daily at the beginning 3 days and every other day on the rest, could suppress tumor growth of female BALB/c nude mice subcutaneously injected with 22Rv1 cells, with a significant decreased expression of PTCH on mRNA level observed. The pancreatic CSCs migration and invasion could be dose-dependently inhibited by 1, 5, 10μM GANT 61 for 24 or 48h, and the decreased expression of c-Myc, Nanog, Sox-2 and Oct-4 on mRNA level could be observed at 36h.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	-	Reduction of GLI2 mediated transcription in HEK293 cells by luciferase reporter assay	17494766
HEK293 cells	-	Function assay	-	Inhibition of beta galactosidase in HEK293 cells	17494766
human 22Rv cells	-	Function assay	-	Reduction of expression of PTCH mRNA in human 22Rv cells	17494766

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动物研究
剂量
Nude Mice: 25 mg/kg^[3] (s.c.), 50 mg/kg^[4] (p.o.)

给药途径
s.c., p.o.

动物研究
剂量	Nude Mice: 25 mg/kg^[3] (s.c.), 50 mg/kg^[4] (p.o.)
给药途径	s.c., p.o.

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
- 2.3277 mL
- 11.6387 mL
- 23.2775 mL
- 5 mM
- 0.4655 mL
- 2.3277 mL
- 4.6555 mL
- 10 mM
- 0.2328 mL
- 1.1639 mL
- 2.3277 mL

技术信息

CAS号

500579-04-4

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

C27H35N5

运输

蓝冰

分子量

429.60

别名

NSC 136476

溶解度

DMSO	Insoluble
Water	Insoluble
Ethanol	12.0 mg/mL (27.9 mM)

动物实验配方

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2,2'-((2-(Pyridin-4-yl)dihydropyrimidine-1,3(2H,4H)-diyl)bis(methylene))bis(N,N-dimethylaniline) Catalog No. CSN15989

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