AZ7550

SKU: orb1708049

Description

AZ7550, the active metabolite of the third-generation EGFR inhibitor AZD9291 (Osimertinib), also functions as an IGF1R inhibitor with an IC50 of 1.6 µM. This compound is a valuable research tool for studying IGF1R signaling in cancer models, applicable in both in vitro biochemical assays and in vivo research exploring resistance mechanisms.

Research Area

Cardiovascular Research, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1421373-99-0
• MW: 485.58
• Purity: 97.07% (May vary between batches)
• Formula: C₂₇H₃₁N₇O₂
• SMILES: CN1C=C(C=2C1=CC=CC2)C3=NC(NC4=C(OC)C=C(N(CCNC)C)C(NC(C=C)=O)=C4)=NC=C3
• Target: BTK,FLT,FAK,PYK2,IGF-1R,MNK,EGFR,ACK1,Drug Metabolite,ALK,MLK,Tyrosine Kinases
• Solubility: DMSO:2.56 mg/mL (5.27 mM)

Bioactivity

• Target IC50:
  BLK:977 nM |Brk:843 nM |Ack1:156 nM |FES:449 nM |FLT3:302 nM |FAK:995 nM |ALK:420 nM |MNK2:228 nM |PYK2:2288 nM |Insulin receptor:1256 nM |IRR:840 nM |TEC:1317 nM |ERB4:195 nM |FLT4:1784 nM |MLK1:88 nM |IGF-1R:1.6 μM
• In Vitro:
  AZ7550 (Compound 28) inhibits double mutant (DM) cell line H1975, activating mutant (AM) cell line PC9, and wild type (WT) cell line LoVo (IC50s: 45, 26, and 786 nM). AZ7550 inhibits DM antiproliferative cell line H1975, AM antiproliferative cell line PC9, and WT antiproliferative cell line Calu3 (GI50s: 19, 15, and 537 nM).

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ALK, ACK1, AZ7550, AZ-7550, BLK, BTK, AZ 7550, Drug Metabolite, DrugMetabolite, BRK, HER1, Ins R, INSR, IGF1R, IGF-1R, EGFR, Epidermal growth factor receptor, FAK, ErbB4, ErbB-1, FES, FLT4, FLT3, Inhibitor, IRR, inhibit, MNK2, MLK1, PYK2, Tyrosine Kinases, TyrosineKinases, Txk, TEC

Compound Identifiers

PubChem CID

71496459