Poziotinib
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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.


Chemical Structure

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Poziotinib
CAS# 1092364-38-9 (free base)

Theoretical Analysis

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

Price and Availability

Size Price Availability Quantity
25.0mg USD 90.0 Ready to ship
50.0mg USD 150.0 Ready to ship
100.0mg USD 250.0 Ready to ship
200.0mg USD 450.0 Ready to ship
500.0mg USD 950.0 Ready to ship
1.0g USD 1650.0 Ready to ship
2.0g USD 2950.0 Ready to ship
5.0g USD 5450.0 2 Weeks
10.0g USD 8650.0 2 Weeks
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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

Appearance: Pale yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: Poziotinib (HM781-36B) is a pan-HER inhibitor, which effectively inhibits EGFRwt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively.
In vitro activity: Poziotinib, a pan-human epidermal growth factor receptor (HER) inhibitor, decreased sphere formation, viability, and proliferation, and induced G1 cell cycle arrest and apoptosis in ovarian CSCs (cancer stem cells). In addition, poziotinib suppressed stemness and disrupted downstream signaling of Wnt/β-catenin, Notch, and Hedgehog pathways, which contribute to many characteristics of CSCs. Interestingly, HER4 was overexpressed in ovarian CSCs and Poziotinib reduced the phosphorylation of STAT5, AKT, and ERK, which are regulated by HER4. Reference: Biochem Biophys Res Commun. 2020 May 21;526(1):158-164. https://www.sciencedirect.com/science/article/abs/pii/S0006291X20305271?via%3Dihub
In vivo activity: The in vivo activity of HM781-36B was assessed in xenograft mice models with various EGFR-dependent cancer cell lines. Daily oral treatments of HM781-36B at 0.3 mg/kg/day or 1 mg/kg/day for 10 days resulted in a dramatic reduction of tumor size with an 83% maximum inhibition rate (mIR, IR = [1 − (relative tumor growth in treated group/relative tumor growth in control group)] × 100) at 0.3 mg/kg/day without body-weight loss. The effect of HM781-36B on HCC827 tumor endothelium was evaluated by immunohistochemistry and a significant reduction in the expression level of pEGFR, pAKT and pERK was observed upon treatment with HM781-36B (0.3 mg/kg/day) for 10 days (Fig. 3b). Reference: Int J Cancer. 2012 May 15;130(10):2445-54. https://onlinelibrary.wiley.com/doi/full/10.1002/ijc.26276

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.0 40.7

Preparing Stock Solutions

The following data is based on the product molecular weight 491.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 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. PMID: 21732342. 2. Lee H, Kim JW, Choi DK, Yu JH, Kim JH, Lee DS, Min SH. Poziotinib suppresses ovarian cancer stem cell growth via inhibition of HER4-mediated STAT5 pathway. Biochem Biophys Res Commun. 2020 May 21;526(1):158-164. doi: 10.1016/j.bbrc.2020.03.046. Epub 2020 Mar 20. PMID: 32201081.
In vitro protocol: 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. PMID: 21732342. 2. Lee H, Kim JW, Choi DK, Yu JH, Kim JH, Lee DS, Min SH. Poziotinib suppresses ovarian cancer stem cell growth via inhibition of HER4-mediated STAT5 pathway. Biochem Biophys Res Commun. 2020 May 21;526(1):158-164. doi: 10.1016/j.bbrc.2020.03.046. Epub 2020 Mar 20. PMID: 32201081.
In vivo protocol: 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. PMID: 21732342.

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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.



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