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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

中文名稱3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
中文同義詞3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺;BCR-ABL抑制劑(GNF-2);化合物GNF-2;3-(6-((4-(三氟甲氧基)苯基)氨基)嘧啶-4-基)苯甲酰胺;GNF-2,BCR-ABL酪氨酸激酶活性的變構(gòu)抑制劑;化合物GNF-2,10 MM DMSO 溶液;GNF-2 (GNF 2;GNF2)
英文名稱GNF-2
英文同義詞3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide GNF-2;GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide;GNF 2, >=98%;3-(6-(4-(TRIFLUOROMETHOXY)PHENYLAMINO)PYRIMIDIN-4-YL)BENZAMIDE;Benzamide, 3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]-;GNF-2;Bcr-abl Inhibitor;3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
CAS號(hào)778270-11-4
分子式C18H13F3N4O2
分子量374.32
EINECS號(hào)200-256-5
相關(guān)類別小分子抑制劑;小分子抑制劑,天然產(chǎn)物;血管生成;細(xì)胞生物學(xué)試劑;標(biāo)準(zhǔn)品;Inhibitors
Mol文件778270-11-4.mol
結(jié)構(gòu)式3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺 結(jié)構(gòu)式

3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺 性質(zhì)

儲(chǔ)存條件2-8°C
溶解度H2O:<2毫克/毫升
形態(tài)白色固體
顏色米白色
水溶解性H2O: <2mg/mL
DMSO: ≥5mg/mL

3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺 用途與合成方法

GNF-2 是一種具有高度選擇性、變構(gòu)的、非 ATP 競(jìng)爭(zhēng)性 Bcr-Abl 抑制劑。 GNF-2 抑制 Ba/F3.p210 增殖, IC50 為 138 nM。

Bcr-Abl

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.

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.

安全信息

危險(xiǎn)品標(biāo)志Xi
危險(xiǎn)類別碼36/37/38
安全說明26
WGK Germany3

MSDS信息

更新日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2025/05/22HY-110073-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
GNF-2
778270-11-41 mg293元
2025/05/22HY-110073-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
GNF-2
778270-11-45mg700元

3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺 上下游產(chǎn)品信息

"3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺"相關(guān)產(chǎn)品信息
卡帕塞替尼 [雙(三氟乙酰氧基)碘]苯 三氯氧磷 4-三氟甲氧基苯基異氰酸酯 GNF-5 GNF-7 PI-103 司美替尼 阿西替尼 曲美替尼 喜樹堿
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