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130306-02-4

中文名稱 (E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE
英文名稱 (E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE
CAS 130306-02-4
分子式 C10H12FN3O4
分子量 257.22
MOL 文件 130306-02-4.mol
130306-02-4 結(jié)構(gòu)式 130306-02-4 結(jié)構(gòu)式

基本信息

中文別名
替扎西他濱
英文別名
tezaciabine
(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE
Cytidine, 2'-deoxy-2'-(fluoromethylene)-, (2'E)-

物理化學(xué)性質(zhì)

沸點(diǎn)512.5±60.0 °C(Predicted)
密度1.71±0.1 g/cm3(Predicted)
儲(chǔ)存條件-80°C
溶解度DMSO : 200 mg/mL (777.54 mM; Need ultrasonic)
酸度系數(shù)(pKa)12.50±0.60(Predicted)
形態(tài)Solid
顏色Off-white to light yellow

常見(jiàn)問(wèn)題列表

生物活性
Tezacitabine 是一種具有細(xì)胞生長(zhǎng)抑制和細(xì)胞毒性的抗代謝藥,是一種核苷類似物。Tezacitabine 不可逆地抑制核糖核苷酸還原酶 (ribonucleotide reductase) 并干擾 DNA 復(fù)制和修復(fù)。Tezacitabine 有效誘導(dǎo)細(xì)胞凋亡 (apoptotic),可用于白血病和實(shí)體瘤的研究。
靶點(diǎn)

Ribonucleotide reductase

體外研究

Tezacitabine (0.01-10 μM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment induces the G1 and S-phase leaky block of the cell cycle.
Tezacitabine (0.01-10 μM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner.
Tezacitabine has strong cytostatic and cytotoxic properties. Cytotoxic effect of Tezacitabine reveals not only as apoptosis, but also as a change in protein metabolism.

Cell Cycle Analysis

Cell Line: CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells
Concentration: 0.01 μM, 0.1 μM, 1.0 μM, and 10 μM
Incubation Time: 24 hours
Result: Induced the G1 (at concentrations higher than 10 nM) and S-phase (at low concentration) leaky block of the cell cycle.

Apoptosis Analysis

Cell Line: CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells
Concentration: 0.01 μM, 0.1 μM, 1.0 μM, and 10 μM
Incubation Time: 24 hours
Result: Induced apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner.
體內(nèi)研究

Tezacitabine (100 mg/kg; intraperitoneal injection; daily; female nude mice) treatment inhibits tumor growth in HCT 116 tumor xenografts.

Animal Model: Female nude mice (7-9-week-old) injected with HCT 116 cells
Dosage: 100 mg/kg
Administration: Intraperitoneal injection; daily; 14 days
Result: Inhibited tumor growth in HCT 116 tumor xenografts.
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