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Poziotinib CAS: 1092364-38-9

Category: Inhibitors
Product Name: Poziotinib
Cat No: I000381
CAS No: 1092364-38-9
Synonyms: 1-(4-((4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one
Molecular Formula: C23H21Cl2FN4O3
Molecular Weight: 491.3
SMILES: O=C(C=C)N1CCC(OC2=CC(C(NC3=C(F)C(Cl)=C(Cl)C=C3)=NC=N4)=C4C=C2OC)CC1
InChI: InChI=1S/C23H21Cl2FN4O3/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27-12-28-23(14)29-16-5-4-15(24)21(25)22(16)26/h3-5,10-13H,1,6-9H2,2H3,(H,27,28,29)
InChIKey: LPFWVDIFUFFKJU-UHFFFAOYSA-N
Solubility: 10 mM in DMSO
Target: HER2
IC50: 3/5/23 nM(HER1/HER2/HER4) [1]
Storage: Store at -20°C
CAS 1092364-38-9,Poziotinib
  • Description

Poziotinib(NOV120101; HM781-36B) is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.
IC50 value: 3/5/23 nM(HER1/HER2/HER4) [1]
Target: pan-HER inhibitor
in vitro: The IC50 levels of HM781-36B for N87 and SNU216 were 0.001 and 0.004 μmol/L, respectively, which was 10–1000 fold lower than the IC50 levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family and downstream proteins, and induced apoptosis and G1 arrest compared to gefitinib or lapatinib [1]. HM781-36B is a potent inhibitor of EGFR in vitro, including the EGFR-acquired resistance mutation (T790M), as well as HER-2 and HER-4, compared with other EGFR tyrosine kinases inhibitors (erlotinib, lapatinib and BIBW2992). HM781-36B treatment of EGFR DelE746_A750-harboring erlotinib-sensitive HCC827 and EGFR L858R/T790M-harboring erlotinib-resistant NCI-H1975 NSCLC cells results in the inhibition of EGFR phosphorylation and the subsequent deactivation of downstream signaling proteins [2]. The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression and SNU-175 cells (IC50 = 0.003 and 0.005 M, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle and apoptosis, and reduced the levels of HER family and downstream signaling molecules, pERK and pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX [3].
in vivo: The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, and tumor volume in mice receiving coadministraion of HM781-36B and 5-FU was smaller than tumor volume in mice receiving HM781-36B only [1].

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:A Phase II Study of Poziotinib in Patients with Epidermal Growth Factor Receptor (EGFR)-Mutant Lung Adenocarcinoma Who Have Acquired Resistance to EGFR-Tyrosine Kinase Inhibitors. Han JY, Lee KH, Kim SW, Min YJ, Cho E, Lee Y, Lee SH, Kim HY, Lee GK, Nam BH, Han H, Jung J, Lee JS.Cancer Res Treat. 2017 Jan;49(1):10-19. doi: 10.4143/crt.2016.058. Epub 2016 May 3. PMID: 27188206 Free PMC Article
2:Population pharmacokinetics of HM781-36 (poziotinib), pan-human EGF receptor (HER) inhibitor, and its two metabolites in patients with advanced solid malignancies. Noh YH, Lim HS, Jung JA, Song TH, Bae KS.Cancer Chemother Pharmacol. 2015 Jan;75(1):97-109. doi: 10.1007/s00280-014-2621-7. Epub 2014 Nov 7. PMID: 25377158


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