PP121|cas 1092788-83-4

Cas No.:	1092788-83-4
Synonyms:	PP 121; PP-121
SMILES:	C1CCC(N2N=C(C3=CN=C4NC=CC4=C3)C3=C(N=CN=C23)N)C1
Formula:	C₁₇H₁₇N₇
M.Wt:	319.36
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47385	PI3K-IN-23	PI3K-IN-23 is an (E)-9-oxooctadec-10-en-12-ynoic acid analogue to promote glucose uptake with an EC50 value of 7.00 μM.
DC47384	PI3Kγ inhibitor 5	PI3Kγ inhibitor 5 is an inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with an IC50 value of 34 nM.
DC47382	MCX 28	MCX 28, a triple PI3K/mTOR/PIM inhibitor, displays low nanomolar activity.
DC47088	Amdizalisib	Amdizalisib is a PI3K inhibitor and used for the research of inflammatory disease, autoimmune disease or cancer.
DC46520	iMDK quarterhydrate	iMDK quarterhydrate, a MDK-positive H441 and H520 lung adenocarcinoma cells inhibitor, suppresses the growth of H441 cells by inhibiting the PI3 kinase (PI3K) pathway and inducing apoptosis. iMDK quarterhydrate decreases MDK-induced migration, angiogenesis of endothelial cells and abrogats the progression and metastasis of NSCLC cells.
DC46457	PI3Kγ inhibitor 4	PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation.
DC46384	PI3K-IN-19 hydrochloride	PI3K-IN-19 hydrochloride is a phosphotidylinositol-3-kinase (PI3K) inhibitor extracted from patent WO2017153220, step 5.
DC46273	740 Y-P TFA	740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
DC46266	PI3K-IN-20	PI3K-IN-20 is a PI3k inhibitor extracted from WO2017101847 A1, compound 1.
DC45823	AZ2	AZ2 is a highly selective PI3Kγ inhibitor. AZ2 can be used for the research of inflammatory and immune diseases.