1092364-38-9 Usage
Description
Poziotinib (HM781-36B) is a novel oral cancer cell inhibitor developed by Seoul Medical University in South Korea in 2008. It is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM, and 23.5 nM for HER1, HER2, and HER4, respectively, and is currently in Phase II/III clinical research. Poziotinib is a TKI that covalently and irreversibly inhibits EGFR and HER2, and is unique because of its small terminal group and flexible quinazoline core. Its small size and flexibility allow it to evade the steric hindrance which affects other EGFR TKIs.
Uses
Used in Oncology:
Poziotinib (HM781-36B) is used as an anticancer agent for the treatment of breast and gastric cancer. It has a strong inhibitory effect on erlotinib and gefitinib EGFR L858R/T790M double mutant cells and is suitable for the treatment of patients with advanced NSCLC with exon 20 mutations in EGFR. It is also valuable for patients with advanced NSCLC who are resistant to first-generation EGFR TKI and T790M/MET negative.
Used in Combination Therapy:
Poziotinib (HM781-36B) is used in combination therapy with 5-fluorouracil, platinum compound, paclitaxel, or gemcitabine, showing a good synergistic inhibitory effect on the overexpression of human epidermis No. 2 (HER2). This makes it a promising option for enhancing the efficacy of existing chemotherapeutic treatments.
Used in Targeted Cancer Therapy:
As a targeted small molecule inhibitor of tyrosine kinase, Poziotinib (HM781-36B) is used for the treatment of gastric, non-small cell lung cancer, and breast cancer, either alone or in combination with other treatments. Its unique structure allows it to effectively target and inhibit specific cancer cell growth pathways, making it a valuable addition to the arsenal of cancer treatments.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1092364-38-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,9,2,3,6 and 4 respectively; the second part has 2 digits, 3 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 1092364-38:
(9*1)+(8*0)+(7*9)+(6*2)+(5*3)+(4*6)+(3*4)+(2*3)+(1*8)=149
149 % 10 = 9
So 1092364-38-9 is a valid CAS Registry Number.
1092364-38-9Relevant articles and documents
SYNTHESIS OF POZIOTINIB DERIVATIVE
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, (2022/03/09)
A method for the synthesis of a compound of Formula (II) is provided. Also disclosed is the salt form of the compound. The method includes the introduction of a piperidinyl moiety in a polar aprotic solvent system, followed by the removal of the protecting group and the acrylation step.
METHOD FOR PREPARING 1-(4-(4-(3,4-DICHLORO-2-FLUOROPHENYLAMINO)-7-METHOXYQUINAZOLIN-6-YLOXY)PIPERIDIN-1-YL)PROP-2-EN-1-ONE
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, (2019/05/07)
The present invention relates to a method for manufacturing a targeted 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a much simple way compared to an existing method by conducting a reaction of a compound of chemical formula 2 and a compound of chemical formula 3, among polar aprotic solvents in the presence of a base.COPYRIGHT KIPO 2019
METHOD FOR PREPARING 1-(4-(4-(3,4-DICHLORO-2-FLUOROPHENYLAMINO)-7-METHOXYQUINAZOLIN-6-YLOXY)PIPERIDIN-1-YL)PROP-2-EN-1-ONE
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, (2014/08/07)
The present invention relates to a novel method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a simpler process as compared with conventional methods by allowing 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol to react with an N-acyl piperidine derivative in an inert polar protic solvent in the presence of a base.
