RK-24466

CAS号

213743-31-8

分子式

C23H22N4O

主要靶点

Src

仅限科研使用

Cat No : CM06530

Print datasheet

Synonyms

inhibit|Lck|Lck 64-509|LckCD|KIN 001-51|Inhibitor|RK 24466|RK24466|RK-24466|Src



产品信息

CAS号 213743-31-8
分子式 C23H22N4O
主要靶点 Src
主要通路 蛋白酪氨酸激酶|血管生成
分子量 370.45
纯度 98.07%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|Lck|Lck 64-509|LckCD|KIN 001-51|Inhibitor|RK 24466|RK24466|RK-24466|Src

靶点活性

Lck (64-509):<1 nM (IC50)|LckCD:2 nM (IC50)

体外活性

RK-24466, a lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, significantly inhibited both VSMC proliferation and migration. RK-24466 suppresses VSMC proliferation and migration via down-regulating the protein kinase B (Akt) and extracellular signal regulated kinase (ERK) pathways, and it significantly decreased the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 and, the phosphorylation of retinoblastoma protein (pRb). Additionally, RK-24466 suppressed the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury. The present study identified RK-24466 as a potent VSMC proliferation and migration inhibitor and warrants further studies to elucidate its more detailed molecular mechanisms, such as its primary target, and to further validate its in vivo efficacy as a therapeutic agent for pathologic vascular conditions, such as restenosis and atherosclerosis[1].

溶解度

DMSO:40 mg/mL (107.97 mM)

参考文献

1.Seo HH, et al. 7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d] pyrimidin-4-ylamine inhibits the proliferation and migration of vascular smooth muscle cells by suppressing ERK and Akt pathways. Eur J Pharmacol. 2017 Mar 5;798:35-42.
2.Arnold LD, et al. 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.

The molarity calculator equation

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

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

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

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2