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839706-07-9

中文名稱 GNF-7
英文名稱 BenzaMide, N-[3-[1,4-dihydro-1-Methyl-7-[(6-Methyl-3-pyridinyl)aMino]-2-oxopyriMido[4,5-d]pyriMidin-3(2H)-yl]-4-Methylphenyl]-3-(trifluoroMethyl)-
CAS 839706-07-9
分子式 C28H24F3N7O2
分子量 547.53
MOL 文件 839706-07-9.mol
更新日期 2024/12/24 19:29:57
839706-07-9 結(jié)構(gòu)式 839706-07-9 結(jié)構(gòu)式

基本信息

中文別名
化合物GNF7
BCR-ABL WT和BCR-ABL T315I抑制劑(GNF-7)
N-[3-[1,4-二氫-1-甲基-7-[(6-甲基-3-吡啶基)氨基]-2-氧代嘧啶并[4,5-D]嘧啶-3(2H)-基]-4-甲基苯基]-3-(三氟甲基)苯甲酰胺
英文別名
GNF-7
CS-1945
GNF-7, >98%
BenzaMide, N-[3-[1,4-dihy...
N-[4-methyl-3-[1-methyl-7-[(6-methylpyridin-3-yl)amino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-3-(trifluoromethyl)benzamide
N-[3-[1,4-Dihydro-1-methyl-7-[(6-methyl-3-pyridinyl)amino]-2-oxopyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide
N-(4-Methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)-3-(trifluoromethyl)benzamide
BenzaMide, N-[3-[1,4-dihydro-1-Methyl-7-[(6-Methyl-3-pyridinyl)aMino]-2-oxopyriMido[4,5-d]pyriMidin-3(2H)-yl]-4-Methylphenyl]-3-(trifluoroMethyl)-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

密度1.404±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度insoluble in EtOH; insoluble in H2O; ≥5.48 mg/mL in DMSO
酸度系數(shù)(pKa)12.82±0.70(Predicted)
形態(tài)固體
顏色White to off-white

圖譜信息

常見問題列表

生物活性
GNF-7 是一種多重激酶抑制劑。GNF-7 是 Bcr-Abl 的抑制劑,對 Bcr-AblWT 和 Bcr-AblT315I 作用的 IC50 值分別為 133 nM 和 61 nM。GNF-7 對 ACK1 和 GCK 也具有抑制活性,IC50 分別為 25 nM 和 8 nM。GNF-7 可用于血液惡性腫瘤的研究。
靶點

IC50: 133 nM (Bcr-Abl WT ), 61 nM (Bcr-Abl T315I ), 25 nM (ACK1), 8 nM (GCK)

體外研究

GNF-7 potently inhibits wild-type Bcr-Abl (IC 50 <5 nM) and Bcr-Abl mutants such as T315I (IC 50 =11 nM), G250E (IC 50 <5 nM), E255V (IC 50 =10 nM), F317L (IC 50 <5 nM) and M351T (IC 50 <5 nM) in cellular assays.
GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream.
GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines.

Western Blot Analysis

Cell Line: Ba/F3-NRAS-G12D cells, OCI-AML3 cells
Concentration: 1 μM
Incubation Time: 2 hours
Result: Caused a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38.

Apoptosis Analysis

Cell Line: OCI-AML3 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1.

Cell Cycle Analysis

Cell Line: OCI-AML3 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Induced of G0-G1 arrest.
體內(nèi)研究

GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model.
GNF-7 exhibits moderate oral bioavailability (mice 36%) and C max (mice 3616 nM) following oral administration (mice 20 mg/kg).
GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg).

Animal Model: 6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft
Dosage: 10 mg/kg, 20 mg/kg
Administration: Oral administration, daily, for 7 days
Result: Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg).
Animal Model: 5-6 weeks old male Balb/c mice (20-25 g)
Dosage: 5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral gavage
Result: Oral bioavailability (36%), C max (3616 nM), T 1/2 (3.2 h).
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