LAS191954|LAS-191954;LAS 191954

Cas No.:	1403947-26-1
Chemical Name:	(S)-2-(1-((6-amino-5-cyanopyrimidin-4-yl)amino)ethyl)-4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazine-5-carbonitrile
Synonyms:	LAS-191954;LAS 191954
SMILES:	N12C=CC(C#N)=C1C(=O)N(C1=CC=CC=C1)C([C@H](NC1C(C#N)=C(N)N=CN=1)C)=N2
Formula:	C₂₀H₁₅N₉O
M.Wt:	397.392801523209
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 of 2.6 nM; displays highest selectivity versus PI3Kα (IC50=8.2 uM) and the lowest versus PI3Kγ and PI3Kβ (IC50=72 and 94 nM respectively); inhibits pAkt (Thr308) produced through PI3K with IC50 of 7.8 nM in THP-1 cells, inhibits IL2 production with an ID50 of 0.13 mg/kg in rat model of con A.

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.
DC45823	AZ2	AZ2 is a highly selective PI3Kγ inhibitor. AZ2 can be used for the research of inflammatory and immune diseases.
DC45809	PKI-179 hydrochloride	PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo.