货号:A145474 同义名: N-(氨基羰基)羟胺 / Hydroxycarbamide;NCI C04831
Hydroxyurea是一种细胞凋亡诱导剂,通过靶向核苷酸还原酶抑制 DNA 合成,还显示出抗正痘病毒活性。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | DNA synthesis ↓ ↑ | helicase ↓ ↑ | RdRp ↓ ↑ | ribonucleotide reductase ↓ ↑ | tRNA synthetase ↓ ↑ | YB-1 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Fexinidazole | ✔ | 98% | |||||||||||||||||
Daptomycin | ✔ | 98% | |||||||||||||||||
Blasticidin S·HCl | ✔ | 98% | |||||||||||||||||
Metronidazole | ✔ | 98% | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Triglycidyl isocyanurate | ✔ | p53 | 98+% | ||||||||||||||||
Nedaplatin | ✔ | 99%+ | |||||||||||||||||
Bendamustine | ✔ | 98+% | |||||||||||||||||
Trifluridine | ✔ | 98% | |||||||||||||||||
Robinetin | ✔ | 99%+ | |||||||||||||||||
Carboplatin | ✔ | 99% | |||||||||||||||||
Cidofovir | ✔ | 99% | |||||||||||||||||
Cisplatin | ✔ | 99% | |||||||||||||||||
Cytarabine |
++++
DNA synthesis, IC50: 16 nM |
98% | |||||||||||||||||
Acelarin |
++++
DNA synthesis, EC50: 0.2 nM |
99%+ | |||||||||||||||||
Oxaliplatin | ✔ | 98% | |||||||||||||||||
YK-4-279 | ✔ | 99%+ | |||||||||||||||||
ML216 |
+
BLMfull-length, IC50: 2.98 μM BLM636-1298, IC50: 0.97 μM |
99%+ | |||||||||||||||||
RK-33 | ✔ | 98% | |||||||||||||||||
Brr2-IN-3 | ✔ | 99%+ | |||||||||||||||||
Phen-DC3 Trifluoromethanesulfonate | ✔ | 98% | |||||||||||||||||
Favipiravir | ✔ | 97% | |||||||||||||||||
Suramin sodium salt |
++
RdRp, IC50: 0.26 μM |
99%+ | |||||||||||||||||
Clofarabine |
++
Ribonucleotide reductase, IC50: 65 nM |
97% | |||||||||||||||||
Didox | ✔ | 98% | |||||||||||||||||
(E)-3-AP | ✔ | 97% | |||||||||||||||||
Halofuginone |
+++
prolyl-tRNA synthetase, Ki: 18.3nM |
99%+ | |||||||||||||||||
BC-LI-0186 |
+++
Leucyl-tRNA synthetase, Kd: 42.1 nM Leucyl-tRNA synthetase, IC50: 46.11 nM |
98% | |||||||||||||||||
SU056 |
+
YB-1, IC50: 1.73 μM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Ribonucleotide reductase (RNR) is an emzyme that catalyses the rate limiting step in the production of deoxyribonucleotides needed for DNA synthesis[1]. RNR inhibitors are a family of anti-cancer drugs because they could affect the growth of tumor cells by interfering the DNA synthesis. Hydroxyurea (HU) is the inhibitor of ribonucleotide reductase (RNR) with IC50 value of 150 μM[2]. The ML L5178 cells, HU treatment at concentrations 0.25 mmol/l resulted in significant increases of DNA damage, detected as strand breaks in the alkaline comet assay [3]. After incubation with 2 mM HU for 4 hours on MCF7 cells, the level of phosphorylated RPA2 measured significantly increased and for 6 hours the percentage of cells with ssDNA was markedly decreased[4]. The pregnant C57BL/6 mice was intraperitoneally injected with 225 mg/kg HU and their embryos were explanted later. The RNR activity decreased significantly after 1 hour and the dNTP level in the brain tissues was attenuated with time[5]. |
作用机制 | The HU is converted into its oxidized form compound III in the radical site of the ribonucleotide reductase protein. The compound III then reacts with the active site residues specially Tyr-176, and inhibits the radical generation and subsequently inhibits the RNR enzyme[6]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
L1210 Leukemia cells | Growth inhibition assay | Concentration required for 50% inhibition of cell growth (L1210 Leukemia), IC50=21.3796 μM | 2991520 | ||
P388 leukemic cell | Proliferation assay | 24-48 h | Antiproliferative activity of compound expressed as concentration that inhibits 50% of growth of P388 leukemic cell suspension from 24 to 48 hr after compound addition, IC50=32 μM | 2709372 |
Dose | Mice: 25 mg/kg - 100 mg/kg[7] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
13.15mL 2.63mL 1.31mL |
65.75mL 13.15mL 6.57mL |
131.49mL 26.30mL 13.15mL |
CAS号 | 127-07-1 |
分子式 | CH4N2O2 |
分子量 | 76.055 |
别名 | N-(氨基羰基)羟胺 ;Hydroxycarbamide;NCI C04831;Droxia;Carbamoyl oxime;Biosupressin;NSC 32065 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 50 mg/mL(657.42 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 50 mg/mL(657.42 mM),配合低频超声助溶 |
动物实验配方 |