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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
PP121是一种作用于PDGFR， Hck， mTOR， VEGFR2， Src和Abl的多靶点抑制剂，IC50分别为2 nM， 8 nM， 10 nM， 12 nM， 14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。An inhibitor of c-Abl, PI 3-kinase, PDGFR, Hck, FRAP, Flk-1, SRC, and DNA-PK.
Information
PP-121 is a multi-targeted inhibitor ofPDGFR, Hck,mTOR,VEGFR2,SrcandAblwithIC50of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibitsDNA-PKwithIC50of 60 nM.
In vitro
PP-121 selectivity interacts within a hydrophobic pocket that is conserved between both tyrosine kinases and PI3Ks, not serine-threonine kinases. PP-121 makes a hydrogen bond to Glu310 in Src, effectively substituting for the structural role of the catalytic lysine and resulting in the ordering of helix C and stabilization of an active conformation. PP-121 also inhibits other PI3Ks including p110α and DNA-PK with IC50 of 52 nM and 60 nM, respectively. PP-121 potently and dose-dependently blocks the phosphorylation of Akt, p70S6K and S6 in two glioblastoma cell lines, U87 and LN229. PP-121 potently inhibits the proliferation of a subset of the tumor cell lines by direct inhibition of PI3Ks and mTOR. PP-121 induces a G0/G1 arrest in LN220, U87 and Seg1 cells. PP-121 also blocks tyrosine phosphorylation induced by v-Src in NIH3T3 cells transformed with v-Src(Thr338). PP-121 could restore actin stress fiber staining in NIH3T3 cells transformed with v-Src(Thr338). PP-121 at a low concentration of 40 nM inhibits Ret autophosphorylation in TT thyroid carcinoma cells that express the C634W oncogenic Ret mutant35. PP-121 inhibits cell proliferation with IC50 of 50 nM in TT thyroid carcinoma cells. PP-121 inhibits cell proliferating stimulated only with VEGF with IC50 of 41 nM in human umbilical vein endothelial cells (HUVECs). PP-121 directly inhibits Bcr-Abl induced tyrosine phosphorylation, resulting in drug-induced apoptosis in K562 cells and a combination of apoptosis and cell cycle arrest in Bcr-Abl expressing BaF3 cells.
In vivo
Cell Data
cell lines：SCLC cell lines NCI-H889, NCI-H1963, NCI-H1417, NCI-H146, NCI-187, DMS79, NCI-1048, NCI-H82, NCI-H196, H69AR, and DMS114
Concentrations：0.04-20 μM
Incubation Time：24-72 hours
Powder Purity:≥99%
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 H2412192 |
分析证书 | P408944 |
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