基本信息

技术规格

物性(参考值)

相关法规

基本信息

产品描述

Cladribine是一种腺苷脱氨酶抑制剂，作用于U266， RPMI8226，和MM1.S细胞，IC50分别约为2.43 μM， 0.75 μM，和0.18 μM。

靶点（IC50 & Targe）

Adenosine deaminase (MM1.S cells),0.18μM

Adenosine deaminase (RPMI8226 cells),0.75μM

Adenosine deaminase (U266 cells),2.43μM

体外研究

Cladribine对毛细胞白血病(HCL)，一种慢性B淋巴细胞增生疾病发挥显著的活性，延长完全缓解期。Cladribine诱导DNA链断裂累积，随后激活淋巴细胞中抑癌基因p53。Cladribine可能调节MM细胞中STAT3活性。Cladribine剂量依赖性抑制U266，RPMI8226和MM1.S细胞的增殖/存活。其中U266对cladribine敏感性最低，而对MM1.S敏感性最高。Cladribine治疗逐渐增加细胞周期中G1期的细胞比例，并减少S期细胞。Cladribine处理24小时后似乎能够增加U266细胞中G2-M期的比例。在RPMI8226和MM1.S细胞中都能观察到cladribine诱导的细胞凋亡剂量依赖性增加。0.2 μM cladribine治疗时间依赖性显著诱导MM1.S 中caspase-3，-8，和-9激活和PARP裂解。Cladribine剂量依赖性显著降低磷酸STAT3 (P-STAT3)水平，但是不影响总STAT3蛋白质水平。[1] Cladribine在HSB2细胞中具有浓度依赖性诱导细胞凋亡的潜能。[2] Cladribine以剂量依赖的方式抑制原代肥大细胞(MC)和MC系HMC-1生长，含有KIT D816V的HMC-1.2细胞与KIT D816V缺失的HMC-1.1细胞相比，具有较低的IC50值。[3] Cladribine降低CD14+单核细胞，以及CD4+和CD8+ T淋巴细胞的迁移能力。[4]

体内研究

Cladribine (0.7-3.5 mM)和/或diltiazem (2.4 mM)，腹腔注射到成年斑马鱼，通过HPLC分析心血管健康的潜在标志物，红血球(RBC)裂解物嘌呤核苷酸(例如ATP)的水平。Diltiazem增加RBC ATP浓度，该作用被共注射cladribine所抑制。[5] Ia 和s.c.给药后，伴随双相下降，Cladribine血浆浓度急速减少。单剂Cladribine 以1 mg/kg ia 和 2 mg/kg s.c. 注射后，AUC和t 1/2β分别为0.66: 1.2 μg ×h/mL和3.5: 4.5小时。[6]

细胞实验

Cell lines: U266，RPMI8226 和 MM1.S

Concentrations: 0 μM - 32 μM

Incubation Time: 72小时

Method: 非放射性细胞增殖试剂盒用于测定细胞活性。简而言之，人MM细胞系U266，RPMI8226和MM1.S接种到96孔板，0.1 mL完全培养基(5% FBS)为对照组，0.1 mL包含一系列剂量cladribine的相同培养基为试验组，培养72小时。使用微板读书器在490 nm下读取所有孔中的细胞数量，每组相对于100%存活率对照组的存活细胞百分数，通过MTS的减少测定。

(Only for Reference)

动物实验

Animal Models: 成年野生型(AB)斑马鱼

Formulation: 生理盐水

Dosages: 0.7 mM - 3.5 mM

Administration: 腹腔注射给药

(Only for Reference)

参考文献

[1] Ma J, et al. BMC Cancer. 2011, 11, 255.

[2] Guchelaar HJ, et al. Cancer Chemother Pharmacol. 1998, 42(1), 77-83.

[3] B?hm A, et al. Exp Hematol. 2010, 38(9), 744-755.

[4] Kopadze T, et al. Eur J Neurol. 2009, 16(3), 409-412.

[5] Klein LC, et al. Biomarkers. 2009, 14(8), 554-559.

[6] Yeung PK, et al. Drug Metabol Drug Interact. 2008, 23(3-4), 291-298.

[7] Szmigielska-Kaplon A, et al. Ann Hematol. 2002, 81(9), 508-5

安全信息

图形或危害标志
提示语	Danger
危险说明	H301 H341 H361fd H372
防范说明	P201 P202 P260 P264 P270 P301+P310
UN号码	2811
危险分类	6.1
包装等级	III
WGK	3
RTECS	AU7357560

基本信息

分子量
285.69

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

包装

Unit quantity: 100 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

注意

Please find SDS provided by EDQM here..

其他说明

Sales restrictions may apply.

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H301 - H341 - H361fd - H372
预防措施声明	P201 - P202 - P260 - P264 - P270 - P301 + P310
危险分类	Acute Tox. 3 Oral - Muta. 2 - Repr. 2 - STOT RE 1
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the Issuing Pharmacopoeia. For further information and support please go to the website of the issuing Pharmacopoeia.

包装

Unit quantity: 10 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

注意

Please find SDS provided by EDQM here..

其他说明

Sales restrictions may apply.

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H301 - H341 - H361fd - H372
预防措施声明	P201 - P202 - P260 - P264 - P270 - P301 + P310
危险分类	Acute Tox. 3 Oral - Muta. 2 - Repr. 2 - STOT RE 1
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

产品说明

应用

2-Chloro-2′-deoxyadenosine (2-CdA) is a chlorinated purine nucleoside with activity against lymphoproliferative disorders, such as hairy cell leukemia (HCL) and multiple myeloma (MM). 2-CdA resists ADA degradation and is phosphorylated to CdATP in lymphocytes. CdATP incorporation into DNA induces strand breaks and the activation of apoptosis. 2-CdA may also be used in studies involving the inhibition of DNA polymerase(s).
Cladribiane, like fludarabine, is a prodrug that is must be phosphorylated intracellularly to the monophosphate by the nuclear/cytosol enzyme deoxycytidine kinase (dCK) and possibly by the mitochondrial enzyme deoxyguanosine kinase (dGK).
Cladribiane, like fludarabine, is a prodrug that is must be phosphorylated intracellularly to the monophosphate by the nuclear/cytosol enzyme deoxycytidine kinase (dCK) and possibly by the mitochondrial enzyme deoxyguanosine kinase (dGK). Clinically used for treatment of hairy cell leukemia, chronic lymphocytic leukemia and other indolent leukemias.

包装

10 mg in poly bottle
25 mg in glass bottle

生化/生理作用

Deoxyadenosine analog resistant to adenosine deaminase; antileukemic with immunosuppressive activity

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H301 - H341 - H361fd - H372
预防措施声明	P201 - P202 - P260 - P264 - P270 - P301 + P310
危险分类	Acute Tox. 3 Oral - Muta. 2 - Repr. 2 - STOT RE 1
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable
个人防护装备	Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

分析说明

These products are for test and assay use only. They are not meant for administration to humans or animals and cannot be used to diagnose, treat, or cure diseases of any kind.  ​

其他说明

USP issued SDS can be found here.
Sales restrictions may apply.

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H301 - H341 - H361fd - H372
预防措施声明	P201 - P202 - P260 - P264 - P270 - P301 + P310
危险分类	Acute Tox. 3 Oral - Muta. 2 - Repr. 2 - STOT RE 1
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

产品说明

一般描述

A deoxyadenosine analog that displays strong antileukemic and immunosuppressive activity. Also induces apoptosis in chronic lymphocytic leukemia (CLL) cells.

包装

10 mg in Plastic ampoule

生化/生理作用

Product does not compete with ATP.
Reversible: no
Cell permeable: no
Primary Target
Antileukemic and immunosuppressive activity

警告

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

其他说明

Bellosillo, B., et al. 1997. Blood 89, 3378; Bryson, H.M., and Sorkin, E.M. 1993. Drugs 46, 872.
Robertson, L.E., et al. 1993. Blood81, 143.
Carson, D.A., et al. 1988. Adv. Enzyme Regul. 27, 395.
Carson, D.A., et al. 1984. Proc. Natl. Acad. Sci. USA 81, 2232.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H301 - H341 - H361fd - H372
预防措施声明	P201 - P202 - P260 - P264 - P270 - P301 + P310
危险分类	Acute Tox. 3 Oral - Muta. 2 - Repr. 2 - STOT RE 1
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

基本信息

安全信息

图形或危害标志
危险性说明	H302: Harmful if swallowed. H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation.
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing P264: Wash hands thoroughly after handling. P270: Do not eat, drink or smoke when using this product. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P301 + P312: IF SWALLOWED: Call a POISON CENTER or doctor/physician if you feel unwell. P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: . P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see . on this label). P330: Rinse mouth. P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to local regulations.