1421373-99-0

1421373-99-0 structure

1421373-99-0 structure

Name: AZ7550
Chemical Name: AZ7550
CAS Number: 1421373-99-0
Molecular Formula: C₂₇H₃₁N₇O₂
Molecular Weight: 485.581
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK IGF-1R
Create Date: 2018-06-14 14:23:03
Modify Date: 2024-02-04 19:16:21
AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.

Name	AZ7550
Synonyms	N-(4-Methoxy-5-{[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino}-2-{methyl[2-(methylamino)ethyl]amino}phenyl)acrylamide 2-Propenamide, N-[4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]-2-[methyl[2-(methylamino)ethyl]amino]phenyl]-

Description	AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IGF-1R Research Areas >> Cancer
Target	IC50: 1.6 μM (IGF1R), 88 nM (MLK1), 156 nM (ACK1), 195 nM (ErbB4), 228 nM (MNK2), 302 nM (FLT3), 420 nM (ALK ), 449 nM (FES), 840 nM (IRR), 843 nM (BRK), 977 nM (BLK), 995 nM (FAK), 1256 nM (Ins R), 1317 nM (TEC), 1784 nM (FLT4), 2288 nM (PYK2), 2443 nM (Txk), 5104 nM (BTK)[1]
In Vitro	AZ7550 (Compound 28) appeares to offer a broadly similar potency and selectivity profile to the parent compound AZD9291. AZ7550 inhibits double mutant (DM) cell line H1975, activating mutant (AM) cell line PC9, and wild type (WT) cell line LoVo with IC50s of 45, 26, and 786 nM, respectively. AZ7550 inhibits DM antiproliferative cell line H1975, AM antiproliferative cell line PC9, and WT antiproliferative cell line Calu3 with GI50s of 19, 15, and 537 nM, respectively[1].
Kinase Assay	Biochemical enzyme profiling of AZD9291 and active metabolites across the kinome panel (single profiling experiment representative of two independent studies). % inhibition for kinases in the ~280 kinase panel that shows greater than 60% inhibition after 1 μM treatment with AZD9291, AZ5104 or AZ7550, and follow-up IC50s where tested, are shown. Kinases with a conserved cysteine in the analogous position within their catalytic domain as Cys797 in EGFR are also shown, highlighted in bold[1].
References	[1]. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.

Density	1.2±0.1 g/cm3
Molecular Formula	C₂₇H₃₁N₇O₂
Molecular Weight	485.581
Exact Mass	485.253937
LogP	3.32
Index of Refraction	1.630
Storage condition	2-8℃