[CAS NO. 1092364-38-9] Poziotinib (HM781-36B)

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PRODUCTS SPECIFICATIONS [1092364-38-9]

Catalog

SLK-S7358

Brand

Selleck

CAS

1092364-38-9

DESCRIPTION [1092364-38-9]

Overview

MDL	MFCD28044290
Molecular Weight	491.34
Molecular Formula	C23H21Cl2FN4O3
SMILES	N(C=1C2=C(C=C(OC)C(OC3CCN(C(C=C)=O)CC3)=C2)N=CN1)C4=C(F)C(Cl)=C(Cl)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0353 mL	10.1763 mL	20.3525 mL
5 mM	0.4071 mL	2.0353 mL	4.0705 mL
10 mM	0.2035 mL	1.0176 mL	2.0353 mL
50 mM	0.0407 mL	0.2035 mL	0.4071 mL

Description

Poziotinib (HM781-36B, NOV120101) is an irreversible pan- inhibitor with of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces and G1 cell cycle arrest. Phase 2.

Targets

HER1 ^[1] (Cell-free assay)	HER2 ^[1] (Cell-free assay)	HER4 ^[1] (Cell-free assay)
3.2 nM	5.3 nM	23.5 nM

In vitro

Poziotinib specifically inhibits the cell growth in HER2 amplified gastric cancer cells, and inhibits the phosphorylation of EGFR and key components of downstream signaling cascades such as STAT3, AKT and ERK. Poziotinib also induces apoptosis and G1 cell cycle arrest by activating the mitochondrial pathway in HER2 amplified gastric cancer cells. Furthermore, Poziotinib also exerts synergistic effects with chemotherapeutic agents in both HER2 amplified and HER2 non-amplified gastric cancer cells.

In vivo

In nude mice bearing N87 human gastric cancer xenografts, Poziotinib (0.5 mg/kg p.o.) alone significantly inhibits the growth of tumors, and coadministraion of Poziotinib and 5-FU causes more effective tumor inhibition. In addition, HM781-36B shows excellent antitumor activity in a variety of EGFR- and HER-2-dependent tumor xenograft models, including erlotinib-sensitive HCC827 NSCLC cells, erlotinib-resistant NCI-H1975 NSCLC cells, HER-2 overexpressing Calu-3 NSCLC cells, NCI-N87 gastric cancer cells, SK-Ov3 ovarian cancer cells and EGFR-overexpressing A431 epidermoid carcinoma cancer cells.

References

[1] Nam HJ, et al. Cancer Lett. 2011, 302(2), 155-165.
[2] Cha MY, et al. Int J Cancer. 2012, 130(10), 2445-2454.

Synonyms

2-Propen-1-one, 1-[4-[[4-[(3,4-dichloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-1-piperidinyl]-

1-[4-[[4-[(3,4-Dichloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-1-piperidinyl]-2-propen-1-one

Poziotinib

1-[4-[4-(3,4-Dichloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]prop-2-en-1-one