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/ Clofarabine

克罗拉滨 /Clofarabine {[allProObj[0].p_purity_real_show]}

货号：A195550 同义名： 氯法拉滨 / Clolar;Evoltra

Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
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Inaccessible (Haz class 6.1), International USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Clofarabine 化学结构 CAS号：123318-82-1
Clofarabine 化学结构
CAS号：123318-82-1
Clofarabine 3D分子结构
CAS号：123318-82-1
Clofarabine 化学结构 CAS号：123318-82-1
Clofarabine 3D分子结构 CAS号：123318-82-1
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Clofarabine 纯度/质量文件 产品仅供科研

货号：A195550 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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 +

BLM636-1298, IC50: 0.97 μM

BLMfull-length, IC50: 2.98 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, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 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。

Clofarabine 生物活性

靶点

  • ribonucleotide reductase

    Ribonucleotide reductase, IC50:65 nM
描述 Clofarabine (CAFdA or CL-F-Ara-a) is a deoxyadenosine analogue compound that has been used in treatment for relapsed or refractory acute lymphoblastic leukemia (see https://www.fda.gov/). Clofarabine can inhibit DNA synthesis through both inhibition of ribonucleotide reductase activity and DNA polymeraseαactivity. The first, clofarabine is phosphorylated by deoxycytidine kinase to clofarabine triphosphate. Clofarabine triphosphate can compete with dATP for incorporation into A sites of the extending DNA strand catalyzed by both human DNA polymeraseα. The second, clofarabine triphosphate is a potent inhibitor of ribonucleotide reductase and thus depletes the dNTP pool primarily of dCTP and dATP. And this further facilitates clofarabine triphosphate incorporated into the DNA[1]. Though inhibition of DNA synthesis is mainly contributed to the anti-tumor effect, the cytotoxicity of clofarabine can be implemented through induction of DNA damage and mitochondrial damage on CLL cells, thus triggering the apoptosis[2].
作用机制 Clofarabine can inhibit DNA synthesis and DNA strands extension through both inhibition of ribonucleotide reductase and DNA polymeraseα.

Clofarabine 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A549 cells Function assay 5 days Cytostatic activity against human A549 cells after 5 days by SRB assay, GI50=0.086 μM 21711054
BT549 cells Cytotoxicity assay 5 days Cytotoxicity against human BT549 cells after 5 days by SRB assay, GI50=0.065 μM 19929004
CCRF-CEM cell lines Cytotoxicity assay Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.05 μM 1732556
DU145 cells Function assay 5 days Cytostatic activity against human DU145 cells after 5 days by SRB assay, GI50=0.125 μM 21711054

Clofarabine 动物研究

Dose Mice[3] (i.p.): min = 20 mg/kg, max = 600 mg/kg
Administration i.p.
Pharmacokinetics
Animal Mice[3]
Dose 20 mg/kg
Administration i.p.
CL/F 2.707 L/h/kg
K21 1.886 (1/h)
V1/F 28.37 L/kg
AUC0→t 6.124 mg/L/h
K12 0.255 (1/h)
T1/2α 0.356 h
K10 0.095 (1/h)
T1/2β 2.395 h

Clofarabine 参考文献

[1]Xie KC, Plunkett W, et al. Deoxynucleotide pool depletion and sustained inhibition of ribonucleotide reductase and DNA synthesis after treatment of human lymphoblastoid cells with 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) adenine. Cancer Res. 1996 Jul 1;56(13):3030-7.

[2]Genini D, Adachi S, et al. Deoxyadenosine analogs induce programmed cell death in chronic lymphocytic leukemia cells by damaging the DNA and by directly affecting the mitochondria. Blood. 2000 Nov 15;96(10):3537-43.

[3]Luan JJ, Zhang YS, et al. Dosing-time contributes to chronotoxicity of clofarabine in mice via means other than pharmacokinetics. Kaohsiung J Med Sci. 2016 May;32(5):227-34.

Clofarabine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.29mL

0.66mL

0.33mL

16.46mL

3.29mL

1.65mL

32.93mL

6.59mL

3.29mL

Clofarabine 技术信息

CAS号123318-82-1
分子式C10H11ClFN5O3
分子量 303.677
别名 氯法拉滨 ;Clolar;Evoltra;Clolar. Abbreviation: CAFdA.;Clofarabine, US brand names: Clofarex;C1-F-Ara-A
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,2-8°C
溶解度

DMSO: 50 mg/mL(164.65 mM)，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
动物实验配方

2% DMSO+30% PEG 300 +1% Tween 80+water 8 mg/mL

Tags: Clofarabine | 123318-82-1 | Nucleoside Antimetabolite/Analog | Autophagy | Ribonucleotide Reductase Inhibitor | Cell Cycle/DNA Damage | Autophagy | Apoptosis | Nucleoside Antimetabolite/Analog | Autophagy | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Clofarabine 纯度/质量文件 | Clofarabine 亚型比较 | Clofarabine 生物活性 | Clofarabine 细胞研究 | Clofarabine 动物研究 | Clofarabine 参考文献 | Clofarabine 实验方案 | Clofarabine 技术信息

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