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143621-35-6

中文名稱 [(3-氨基吡啶-2-基)亞甲基氨基]硫脲
英文名稱 3-aminopyridine-2-carboxaldehyde thiosemicarbazone
CAS 143621-35-6
分子式 C7H9N5S
分子量 195.24
MOL 文件 143621-35-6.mol
更新日期 2024/06/17 17:25:38
143621-35-6 結(jié)構(gòu)式 143621-35-6 結(jié)構(gòu)式

基本信息

中文別名
3-氨基吡啶-2-甲醛氨基硫脲腙
M2亞基抑制劑(TRIAPINE)
2-[(3-氨基吡啶-2-基)亞甲基]氨基硫脲
PAN-811)是核糖核苷酸還原酶抑制劑,已進(jìn)入各種臨床實(shí)驗(yàn)。
英文別名
Pan811
3-Apct
Pan-811
Pan 811
C078157
OCX 191
CS-2006
Triapine
OCX 0191
NSC 663249
所屬類別
醫(yī)藥中間體:氨基吡啶

物理化學(xué)性質(zhì)

熔點(diǎn)234 °C
沸點(diǎn)436.0±55.0 °C(Predicted)
密度1.46±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度DMSO:可溶10Meq/mL,澄清
酸度系數(shù)(pKa)10.93±0.70(Predicted)
形態(tài)粉末
顏色白色至淺棕色
CAS 數(shù)據(jù)庫143621-35-6

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H301-H315-H319-H335
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類別碼22-36/37/38
安全說明26
危險(xiǎn)品運(yùn)輸編號UN 2811 6.1 / PGIII
WGK Germany3
海關(guān)編碼2933.39.6190
毒性LDLo ivn-rat: 20 mg/kg IJTOFN 19,85,2000
[(3-氨基吡啶-2-基)亞甲基氨基]硫脲價(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2024/11/08HY-10082[(3-氨基吡啶-2-基)亞甲基氨基]硫脲
3-AP
143621-35-65 mg520元
2024/11/08HY-10082[(3-氨基吡啶-2-基)亞甲基氨基]硫脲
3-AP
143621-35-610 mM * 1 mLin DMSO572元
2024/11/08HY-10082[(3-氨基吡啶-2-基)亞甲基氨基]硫脲
3-AP
143621-35-610 mg820元

常見問題列表

生物活性
3-AP (PAN-811) 是一種核糖核苷酸還原酶 (ribonucleotide reductase,RR) 的 M2 亞基抑制劑,是有效的放射致敏劑。
靶點(diǎn)

Ribonucleotide reductase (RR)

體外研究

3-AP (Triapine) is a potent derivative of α-heterocyclic carboxaldehyde thiosemicarbazone (HCT) that inhibits hRRM2 and p53R2 isoforms of the M2 subunit. 3-AP (Triapine) is thought to inhibit ribonucleotide reductase through its preformed iron chelate, rather than directly by removing iron from the active site. In cells containing less topoisomerase IIα fewer DNA strand breaks will be produced, and thus topoisomerase II poisons will be less inhibitory in the K/VP.5 cell line. The IC 50 s for Dp44mT growth inhibition are 48±9 nM and 60±12 nM, for K562 and K/VP.5 cells, respectively. The IC 50 s for 3-AP growth inhibition are 476±39 nM and 661±69 nM for K562 and K/VP.5 cells, respectively. PKIH and DpT Fe chelators show high antiproliferative activity against a range of tumor cell lines. Dp44mT shows the greatest antitumor efficacy with an IC 50 that ranged from 0.005 to 0.4 μM. The average IC 50 of Dp44mT over 28 cell types is 0.03±0.01 μM, which is significantly lower than that of 3-AP (Triapine; average IC 50 : 1.41±0.37 μM).

體內(nèi)研究

3-AP (Triapine) causes a significant increase (1.7-fold) in splenic weight when expressed as a percentage of total body weight (1.02±0.06%; n=25) compared with control mice (0.6±0.03%; n=27). In the long-term group, a significant increase in heart weight is observed after Dp44mT (0.4 mg/kg per day) (0.8±0.06%; n=4) compared with control mice (0.5±0.01%; n=6). A significant decrease in the expression of Ndrg1, TfR1, and VEGF1 in the liver is noted for Dp44mT- and 3-AP (12 mg/kg per day)-treated animals. The decreased expression could be related to the increased liver Fe in both Dp44mT- and 3-AP-treated mice.

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