|7-环戊基-5-(4-苯氧基苯基)-7H-吡咯并[2,3-d]嘧啶-4-胺|CsnPharm

CAS No.: 213743-31-8

RK-24466 Catalog No. CSN23720

Synonyms: KIN 001-51;LCK Inhibitor;Lymphocyte-specific Protein Tyrosine Kinase

RK-24466 is an inhibitor of Lck (64-509) and LckCD isoforms with IC50s of <2 nM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Lck is a src-family tyrosine kinase that predominantly expressed in T lymphocytes. The inhibition of lck activity prevents the activation of T cells, which might be used for the treatment of T-cell-dependent diseases. RK 24466 is a pyrrolopyrimidine that inhibits the activity of two forms of lck kinase, lck (64-509) and lckcd, with IC₅₀ values of <1 nM and 2 nM, respectively. It also blocks kinases scr, kdr, and tie-2 with IC₅₀ values of 0.07, 1.57, and 1.98 µM, respectively. RK 24466 showed much less inhibitory effect on the activities of EGFR, Zap70, PKC, and CDC2/CyB with IC₅₀s values of 3.2 µM, >50 µM, >33 µM, and >50 µM, respectively^[1]. The i.p. administration of RK 24466 at low doses (ED50 = 4 mg/kg) inhibited T-cell receptor-stimulated IL-2 production in mice, while the efficacy was remarkably decreased after the oral administration (ED50 = 25 mg/kg)^[2].
作用机制RK 24466 is a potent and selective inhibitor of lck kinase. The hydrophobic pocket in lck (64-509) is occupied by the phenoxyphenyl moiety of RK 24466, resulting in an increased potency against lck (64-509).
参考文献

[1] Arnold LD, Calderwood DJ, Dixon RW, Johnston DN, Kamens JS, Munschauer R, Rafferty P, Ratnofsky SE. Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70. doi: 10.1016/s0960-894x(00)00441-8. PMID: 11012021.
[2] Burchat AF, Calderwood DJ, Hirst GC, Holman NJ, Johnston DN, Munschauer R, Rafferty P, Tometzki GB. Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2171-4. doi: 10.1016/s0960-894x(00)00442-x. PMID: 11012022.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6994 mL
- 13.4971 mL
- 26.9942 mL
- 5 mM
- 0.5399 mL
- 2.6994 mL
- 5.3988 mL
- 10 mM
- 0.2699 mL
- 1.3497 mL
- 2.6994 mL

技术信息

CAS号

213743-31-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H22N4O

运输

蓝冰

分子量

370.45

别名

KIN 001-51;LCK Inhibitor;Lymphocyte-specific Protein Tyrosine Kinase;KIN001-051

溶解度

DMSO	20.0 mg/mL (54.0 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (13.5 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

RK-24466 Catalog No. CSN23720

靶点选择性

请登录您的专属账户

确认信息