3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺 GNF-2 CAS#:778270-11-4

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首页化工产品目录 3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺

3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺

产品纠错

CAS号：778270-11-4 | 英文名称：GNF-2

分子式 C₁₈H₁₃F₃N₄O₂

分子量 374

EINECS号 200-256-5

MDL MFCD09265253

Smiles

InChIKey

乙二醇化学百科

基本信息

中文名称	3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
英文名称	GNF-2
CAS号	778270-11-4
分子式	C18H13F3N4O2
分子量	374.32
EINECS号	200-256-5

物化性质

溶解度	H2O：<2毫克/毫升
形态	白色固体
颜色	米白色

安全信息

危险品标志	Xi
危险类别码	36/37/38
安全说明	26
WGK Germany	3

生产及用途

生物活性

GNF-2 是一种具有高度选择性、变构的、非 ATP 竞争性 Bcr-Abl 抑制剂。 GNF-2 抑制 Ba/F3.p210 增殖， IC50 为 138 nM。

靶点

Bcr-Abl

体外研究

GNF-2 selectively inhibits Bcr-abl-dependent cell proliferation. GNF-2 (0.005-10 μM; 48 hours) specifically inhibits the proliferation of the Bcr-abl-expressing cells with an IC ₅₀ of 138 nM and not show any cytotoxic effects on the nontransformed cells at concentrations of up to 10 μM. GNF-2 (0.005-10 μM; 48 hours) causes a dose-dependent growth inhibition of the Bcr-abl-positive cell lines with IC ₅₀ values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 (0.005-10 μM; 48 hours) inhibits E255V and Y253H mutant Bcr-abl cell growth (IC ₅₀ values of 268 and 194 nM, respectively).
GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells.
GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC ₅₀ of 267 nM.

Cell Proliferation Assay

Cell Line:	Ba/F3.p210, Ba/F3.p210 ^E255V and Ba/F3.p185 ^Y253H cells
Concentration:	0.005, 0.01, 0.1, 1, 10 μM
Incubation Time:	48 hours
Result:	Inhibited Bcr-abl-transformed cells proliferation.

Apoptosis Analysis

Cell Line:	Ba/F3.p210 and Ba/F3.p210 ^E255V cells
Concentration:	1, 10 μM
Incubation Time:	48 hours
Result:	Increased number of Ba/F3.p210 cells undergoing apoptosis at 1 μM for 48 h. Ba/F3.p210 ^E255V underwent apoptotic death after 48 h incubation in the presence of 1 μM or higher concentration.

Western Blot Analysis

Cell Line:	Ba/F3.p210 and Ba/F3.p210 ^E255V cells
Concentration:	0.1, 1, 10 μM
Incubation Time:	90 minutes
Result:	Decreased the autophosphorylation levels at a concentration of 1 μM and were barely detectable at 10 μM, whereas the level of total Bcr-abl remained unchanged. Induced a significant decrease in the levels of p-Stat5 (at Y694) at 1 μM in Ba/F3.p210 and Ba/F3.p210 ^E255V cells.

体内研究

GNF-2 (10 mg/kg; i.p. for 8 days) protects LPS (5 mg/kg) induced bone erosion in mice. GNF-2 protects the LPS induced bone loss and abrogates the LPS-induced decreases of bone volume/tissue volume (BV/TV) of LPS-treated mice.
GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS.

Animal Model:	Eight-week-old C57/BL6 mice were administered i.p. injections of LPS (5 mg/kg)
Dosage:	10 mg/kg
Administration:	I.p. injections for 8 days; 1 day before and every day after the LPS injection
Result:	Prevented inflammatory bone destruction in vivo.

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