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213743-31-8

中文名稱 213743-31-8
英文名稱 7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR
CAS 213743-31-8
分子式 C23H22N4O
分子量 370.45
MOL 文件 213743-31-8.mol
更新日期 2024/11/08 11:24:23
213743-31-8 結(jié)構(gòu)式 213743-31-8 結(jié)構(gòu)式

基本信息

中文別名
化合物RK-24466
英文別名
RK-24466
KIN 001-51
d]pyrimidin-4-ylamine
RK-24466
RK 24466
RK24466
7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR
Lck Inhibitor - CAS 213743-31-8 - Calbiochem
7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3‑
7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-cyclopentyl-5-(4-phenoxyphenyl)-
7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3‑:d]pyrimidin-4-ylamine

物理化學(xué)性質(zhì)

沸點(diǎn)605.1±55.0 °C(Predicted)
密度1.30±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMSO: 17 mg/mL at ≤60 °C, soluble
酸度系數(shù)(pKa)5.75±0.30(Predicted)
形態(tài)白色固體
顏色white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
WGK Germany3
213743-31-8價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-108318213743-31-8
RK-24466
213743-31-81mg600元
2024/11/08HY-108318213743-31-8
RK-24466
213743-31-85mg1500元
2024/11/08S0020213743-31-8
RK 24466
213743-31-85mg2370元

常見問題列表

生物活性
RK-24466 (KIN 001-51, Lck inhibitor C 8863, C8863)是一種有效的、選擇性的 Lck 抑制劑,可抑制人Lck激酶的兩種構(gòu)建體,lck (64-509)和lckcd,對(duì)應(yīng)的IC50值分別為小于0.001 μM和0.002 μM。
靶點(diǎn)
TargetValue
Lck (64-509)
(Cell-free assay)
0.001 μM
Lckcd
(Cell-free assay)
0.002 μM
體外研究

RK-24466 is selective for Lck over a range of receptor, non-receptor tyrosine kinases and seronine/threonine kinases. RK-24466 are potent inhibitors of IL2 production in Jurkat cells stimulated with anti-CD3 antibody, being at least 100-fold more potent than PP1. RK-24466 displays remarkable cellular selectivity. RK-24466 significantly inhibits 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 decreases the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 and, the phosphorylation of retinoblastoma protein (pRb).

體內(nèi)研究

RK-24466 inhibits T-cell receptor stimulated (a-CD3 mAb) IL-2 production in mice at low doses (ED 50 =4 mg/kg) after ip administration. However, efficacy is greatly reduced after oral administration (ED 50 =25 mg/kg) which is presumed to reflect poor intestinal absorption in the latter regimen. Inhibition of antigen specific T-cell immune responses is also seen for RK-24466. After administration of RK-24466 twice daily (100 mg/kg po) for 3 days during the in vivo priming phase, a 70% inhibition of IFNγ production is seen upon subsequent antigen-specific (KLH) challenge of lymphocytes from the draining lymph nodes in vitro . RK-24466 suppresses the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury.

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