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Cladribine
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Cladribine图片
CAS NO:4291-63-8
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
克拉屈滨
2-Chloro-2′-deoxyadenosine
CldAdo
2CdA
产品介绍
Cladribine (2-Chloro-2′-deoxyadenosine) 是一种嘌呤核苷类似物，是具有口服活性的腺苷脱氨酶 (adenosine deaminase) 抑制剂。Cladribine 能作为 DNA 合成 (DNA synthesis) 的抑制剂，可阻断受损 DNA 的修复。Cladribine 可以抑制 DNA 甲基化。Cladribine 具有抗淋巴瘤活性，可用于一些血液恶性肿瘤和多发性硬化的研究。
生物活性

Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally activeadenosine deaminaseinhibitor. Cladribine functions as an inhibitor ofDNA synthesisto block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis[1][2].

IC50& Target

Adenosine deaminase[2]

体外研究
(In Vitro)

Cladribine (0.25-4 μM; 24-48 hours) inhibits human DLBCL cells proliferation[1].
Cladribine (1-4 μM; 24 hours) induces G1 phase arrest via decreasing the expressions of Cyclin D1 and Cyclin E, and increasing the expressions of p21 and p27 in DLBCL cells[1].
Cladribine (1-4 μM; 24 hours) induces apoptosis and activates extrinsic and intrinsic signaling pathways in human DLBCL cells[1].
Cladribine (1-4 μM; 24 hours) activates endoplasmic reticulum stress[1].
Cladribine inhibits cell proliferation of multiple myeloma (MM) cells in a dose-dependent manner; with IC50s of approximately 2.43 μM, 0.75 μM and 0.18 μM for U266, RPMI8226 and MM1.S cells, respectively[2].

Cell Proliferation Assay[1]

Cell Line:The human DLBCL cell lines (U2932, OCI-LY10, SUDHL2, WSU-DLCL2, DB)
Concentration:0 μM, 0.25 μM, 0.5 μM, 1 μM, 2 μM, 4 μM
Incubation Time:24 hours, 48 hours
Result:Exhibited notable suppression of cell proliferation in five DLBCL cells.

Western Blot Analysis[1]

Cell Line:U2932 cells, WSU-DLCL2 cells
Concentration:0 μM, 1 μM, 2 μM, 4 μM
Incubation Time:24 hours
Result:Decreased the expressions of Cyclin D1 and Cyclin E, and increased the expressions of p21 and p27.

Apoptosis Analysis[1]

Cell Line:U2932 cells, WSU-DLCL2 cells
Concentration:0 μM, 1 μM, 2 μM, 4 μM
Incubation Time:24 hours
Result:Induced apoptosis and activates exogenous and endogenous apoptotic signaling pathways.

Cell Cycle Analysis[1]

Cell Line:U2932 cells, WSU-DLCL2 cells
Concentration:0 μM, 1 μM, 2 μM, 4 μM
Incubation Time:24 hours
Result:Caused G1 phase arrest.

RT-PCR[1]

Cell Line:U2932 cells, WSU-DLCL2 cells
Concentration:0 μM, 1 μM, 2 μM, 4 μM
Incubation Time:24 hours
Result:Activated ER stress.
体内研究
(In Vivo)

Cladribine (10 μg/kg; i.p.; 3 times/week; for 2 weeks) may have benefits in the treatment of ischemia/reperfusion injury to the biochemical and histopathologic parameters[3].
Cladribine (0.5 mg/kg; i.p.; daily; for 60 days) increases amyloid beta peptide generation and plaque burden in APdE9 mice[4].
Cladribine exhibits Cmax(rat 4.9 ng/mL) following intra-arterial injection[5].
Cladribine exhibits Cmax(rat 1.1 ng/mL) following subcutaneous injection[5].
Cladribine exhibits elimination half-lives (rat 3.5 h) and plasma clearance (rat 2.8 L/h/kg) following intra-arterial injection[5].
Cladribine exhibits elimination half-lives (rat 4.5 h) and plasma clearance (rat 2.3 L/h/kg) following subcutaneous injection[5].
Cladribine administration with s.c. injection may produce more favourable pharmacokinetic profiles than i.a. injection following a single dose[5].

Animal Model:Male Sprague-Dawley rats, ischemic injury model[3]
Dosage:10 μg/kg
Administration:Intraperitoneal injection, 3 times/week, for 2 weeks
Result:Might increase expression of Sphk1 and consecutively SphK1 suppressed HIF-1α.
Animal Model:Male Sprague Dawley rats (350-450 g)[5]
Dosage:2 mg/kg for s.c., 1 mg/kg for i.a. (Pharmacokinetic Analysis)
Administration:Subcutaneous injection, intra-arterial
Result:Cmax(4.9 ng/mL i.a.; 1.1 ng/mL s.c.), T1/2β (3.5 h i.a.; 4.5 s.c.).
Clinical Trial
分子量

285.69

性状

Solid

Formula

C10H12ClN5O3

CAS 号

4291-63-8

中文名称

克拉屈滨

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : ≥ 30 mg/mL(105.01 mM)

H2O : 10 mg/mL(35.00 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.5003 mL17.5015 mL35.0030 mL
5 mM0.7001 mL3.5003 mL7.0006 mL
10 mM0.3500 mL1.7501 mL3.5003 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： PBS

    Solubility: 25 mg/mL (87.51 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。