基本信息

技术规格

物性(参考值)

安全信息

图形或危害标志
信号词	警告
危险性说明	H361 : 怀疑对生育能力或胎儿造成伤害。
防范说明	P501 : 将内装物/容器送到批准的废物处理厂处理。 P202 : 在阅读并明了所有安全措施前切勿搬动。 P201 : 使用前取得专用说明。 P280 : 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P308 + P313 : 如接触到或有疑虑：求医/就诊。 P405 : 存放处须加锁。

相关法规

基本信息

产品描述

Nelarabine 一种嘌呤核苷类似物，抑制DNA合成，IC50为0.067-2.15 μM。

靶点（IC50 & Targe）

DNA synthesis (ALL-SIL cells),1.24μM

DNA synthesis (HSB2 cells),0.44μM

DNA synthesis (JURKAT cells),2.15μM

DNA synthesis (PER-255 cells),67nM

通过腺苷脱氨酶的脱甲基化作用，Nelarabine快速转化为ara-G 。

体外研究

Nelarabine在T细胞系和B细胞系中的IC50分别比ARAC高25倍和113倍。T-ALL细胞对Nelarabine的敏感性比B细胞系高8倍，但是有相当大的重叠。NEL在T细胞系和B细胞系中的效能分别比ARAC低25倍和113倍。[1] Nelarabine通过抑制易感细胞中DNA合成，并诱导细胞凋亡发挥作用。[2] Nelarabine具有显著的抗肿瘤活性和可接受的毒性。[3]

体内研究

Nelarabine血浆AUC为2.82 mM分钟，ara-G血浆AUC为20 mM分钟。Nelarabine在血浆中的终末半衰期为25分钟，清除率为42 mL/min/kg，中心分布容积为1.1 L/kg。Ara-G在血浆中的终末半衰期为182分钟，中心分布容积为1.4 L/kg。在CSF中，Nelarabine的终末半衰期为77分钟，而ara-G的终末半衰期为232分钟。Nelarabine的脑脊液分布容积/血浆分布容积为29%，ara-G的为23%。由于Nelarabine和ara-G相当短的半衰期，每日注射不会积累。[4]

细胞实验

Cell lines: HSB2，ALL-SIL，JURKAT 和 PER-255 细胞系

Concentrations: 0.125 μg/mL - 8 μg/mL

Incubation Time: 96小时

Method: HSB2，ALL-SIL，JURKAT和PER-255细胞系使用MTT试验测试耐药性。Nelarabine培养4天以上，测试浓度重复3份。以IC50(抑制50%细胞生长的药物浓度)作为耐药性的量度。数据代表2-6个不同条件下进行的实验的平均值。为避免个别实验中即使在最高剂量下也不能实现50%的细胞毒性，IC50以测试的最高浓度的两倍记录。

(Only for Reference)

动物实验

Animal Models: 健康成年雄性猕猴

Formulation: 水中溶解

Dosages: 35 mg/kg

Administration: 静脉注射给药

(Only for Reference)

参考文献

[1] Beesley AH, et al. Br J Haematol. 2007, 137(2), 109-116.

[2] Kline J, et al. Expert Opin Pharmacother. 2006, 7(13), 1791-1799.

[3] DeAngelo DJ, et al. Blood. 2007, 109(12), 5136-5142.

[4] Berg SL, et al. Cancer Chemother Pharmacol. 2007, 59(6),

安全信息

图形或危害标志
提示语	Warning
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III

产品说明

包装

10, 50 mg in glass bottle

生化/生理作用

Nelarabine is an antineoplastic purine nucleoside analog used in T-cell acute lymphoblastic leukemia. It is a pro-drug of Ara-G, which is converted by cellular kinases to the active 5′-triphosphate, Ara-GTP. Incorporation of Ara-GTP into DNA leads to inhibition of DNA synthesis and apoptosis.

基本信息

产品性质

安全信息

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: Remove victim to fresh air and keep at rest in a position comfortable for breathing.. 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 relevant procedures. 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 in accordance with local regulation .