Cladribine - CAS:4291-63-8

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Cladribine (Synonyms:克拉屈滨; 2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA)

目录号 : KM4644 CAS No. : 4291-63-8 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to 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.

体外研究

Cladribine (0.25-4 μM; 24-48 hours) inhibits human DLBCL cells proliferation.
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.
Cladribine (1-4 μM; 24 hours) induces apoptosis and activates extrinsic and intrinsic signaling pathways in human DLBCL cells.
Cladribine (1-4 μM; 24 hours) activates endoplasmic reticulum stress.
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.

Cell Proliferation Assay

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

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

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

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

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

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.
Cladribine (0.5 mg/kg; i.p.; daily; for 60 days) increases amyloid beta peptide generation and plaque burden in APdE9 mice.
Cladribine exhibits C_max (rat 4.9 ng/mL) following intra-arterial injection.
Cladribine exhibits C_max (rat 1.1 ng/mL) following subcutaneous injection.
Cladribine exhibits elimination half-lives (rat 3.5 h) and plasma clearance (rat 2.8 L/h/kg) following intra-arterial injection.
Cladribine exhibits elimination half-lives (rat 4.5 h) and plasma clearance (rat 2.3 L/h/kg) following subcutaneous injection.
Cladribine administration with s.c. injection may produce more favourable pharmacokinetic profiles than i.a. injection following a single dose.

Animal Model:	Male Sprague-Dawley rats, ischemic injury model
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)
Dosage:	2 mg/kg for s.c., 1 mg/kg for i.a. (Pharmacokinetic Analysis)
Administration:	Subcutaneous injection, intra-arterial
Result:	C_max (4.9 ng/mL i.a.; 1.1 ng/mL s.c.), T_1/2 β (3.5 h i.a.; 4.5 s.c.).

分子式

C₁₀H₁₂ClN₅O₃

分子量

285.69

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 mg	5 mg	10 mg

1 mM	3.5003 mL	17.5015 mL	35.0030 mL
5 mM	0.7001 mL	3.5003 mL	7.0006 mL
10 mM	0.3500 mL	1.7501 mL	3.5003 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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation