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MedKoo CAT#: 205846
CAS#: 1092364-38-9 (free base)
Description: Poziotinib , also known as HM781-36B and NOV120101, is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity. HM781-36B irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. EGFRs, cell surface receptor tyrosine kinases, are often upregulated in a variety of cancer cell types and play key roles in cellular proliferation and survival.
MedKoo Cat#: 205846
Name: Poziotinib
CAS#: 1092364-38-9 (free base)
Chemical Formula: C23H21Cl2FN4O3
Exact Mass: 490.09747
Molecular Weight: 491.34
Elemental Analysis: C, 56.22; H, 4.31; Cl, 14.43; F, 3.87; N, 11.40; O, 9.77
Related CAS #: 1092364-38-9 (free base) 1429757-68-5 (HCl) 1352121-00-6 (x HCl) 1352121-01-7 (phosphate) 1352121-02-8 (sulfate) 1352121-09-5 (besylate) 1352121-06-2 (citrate) 1352121-05-1 (maleate) 1352121-04-0 (malate) 1352121-07-3 (fumarate)
Synonym: HM781-36B; HM78136B; HM-78136B; HM 78136B; NOV120101; NOV-120101; NOV 120101; Poziotinib
IUPAC/Chemical Name: 1-(4-((4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one
InChi Key: LPFWVDIFUFFKJU-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=O
1: Cha MY, Lee KO, Kim M, Song JY, Lee KH, Park J, Chae YJ, Kim YH, Suh KH, Lee GS, Park SB, Kim MS. Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models. Int J Cancer. 2012 May 15;130(10):2445-54. doi: 10.1002/ijc.26276. Epub 2011 Aug 24. PubMed PMID: 21732342.
2: Nam HJ, Kim HP, Yoon YK, Hur HS, Song SH, Kim MS, Lee GS, Han SW, Im SA, Kim TY, Oh DY, Bang YJ. Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer. Cancer Lett. 2011 Mar 28;302(2):155-65. PubMed PMID: 21306821.