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Poziotinib (HM781-36B)

Description In vitro Description In vivo Application
Poziotinib (HM781-36B)
Poziotinib (HM781-36B) structure
CAS No.
1092364-38-9
Chemical Name:
Poziotinib (HM781-36B)
Synonyms
CS-1788;NOV120101;HM781-36B);Poziotinib;UNII-OEI6OOU6IK;Poziotinib(NOV120101;Poziotinib HM-781368;poziotinib(HM-78136B);Poziotinib (HM781-37B);HM781-36B; NOV120101; NOV-120101; NOV 120101; POZIOTINIB
CBNumber:
CB22668103
Molecular Formula:
C23H21Cl2FN4O3
Formula Weight:
491.34
MOL File:
1092364-38-9.mol

Poziotinib (HM781-36B) Properties

Boiling point:
629.7±55.0 °C(Predicted)
Density 
1.409±0.06 g/cm3(Predicted)
pka
5.35±0.30(Predicted)
CAS DataBase Reference
1092364-38-9
FDA UNII
OEI6OOU6IK
NCI Drug Dictionary
poziotinib

Poziotinib (HM781-36B) price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 22437 Poziotinib ≥95% 1092364-38-9 1mg $27 2021-03-22 Buy
Cayman Chemical 22437 Poziotinib ≥95% 1092364-38-9 5mg $74 2021-03-22 Buy
Cayman Chemical 22437 Poziotinib ≥95% 1092364-38-9 10mg $122 2021-03-22 Buy
Cayman Chemical 22437 Poziotinib ≥95% 1092364-38-9 25mg $270 2021-03-22 Buy

Poziotinib (HM781-36B) Chemical Properties,Uses,Production

Description

Poziotinib (HM781-36B) 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. Phase 2.

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.

Description

Poziotinib [1. {4. [4. (3,4. Dichloro.2.monofluoroaniline) -7-methoxyquinazoline-6. Oxygen]. 1. Piperidinyl} propan-2-ene-1one (1)] is a novel oral cancer cell inhibitor developed by Seoul Medical University in South Korea in 2008. It is used for the treatment of breast and gastric cancer, and has targeted Small molecule inhibitor of tyrosine kinase. It is currently in Phase II / III clinical research and can be used alone or in combination for the treatment of gastric, non-small cell lung cancer and breast cancer. Poziotinib is resistant to erlotinib and gefitinib EGFR L858R / T790M Double mutant cells have a strong inhibitory effect.
The combined use of Poziotinib (HM781-36B) and 5-fluorouracil, platinum compound, paclitaxel or gemcitabine shows a good synergistic inhibitory effect on the overexpression of human epidermis No. 2 (HER2). A new third-generation anti-tumor cell inhibitor following the kinase inhibitor afatinib.

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.

Application

Poziotinib is suitable for the treatment of patients with advanced NSCLC with exon 20 mutations in EGFR. Multiple patients have proven effective. Poziotinib is also valuable for patients with advanced NSCLC who are resistant to first-generation EGFR TKI and T790M / MET negative. There are no clinical data on the treatment of patients with brain metastases by Poziotinib. One patient with advanced NSCLC with exon 20 mutation in EGFR had meningeal metastases. This patient has been taking Poziotinib for effective control for 4 months.

Description

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 [138].

Poziotinib (HM781-36B) Preparation Products And Raw materials

Raw materials

Preparation Products


Poziotinib (HM781-36B) Suppliers

Global( 156)Suppliers
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Jurong Coupling Biotechnology Co., Ltd.
13656108824
coupling278191416@hotmail.com CHINA 184 58
ATK CHEMICAL COMPANY LIMITED
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+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26762 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29954 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
Accela ChemBio Inc.
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(+1)-858-876-1948 info@accelachem.com United States 19969 58
Chongqing Chemdad Co., Ltd
+86-13650506873
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Shenzhen Excellent Biotech Co., Ltd.
13480692018
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Zhuozhou Wenxi import and Export Co., Ltd
+8613111626072 (WhatsApp)
Wechat: +8613111626072 Wickr me: waynehu zzwenxi@126.com CHINA 13187 58
Neostar United (Changzhou) Industrial Co., Ltd.
+0086-519-85557386
+0086-519-85557389 marketing1@neostarunited.com CHINA 4135 58
Target Molecule Corp
18019718960 781-999-5354
marketing@targetmol.com United States 19232 58

Related articles


View Lastest Price from Poziotinib (HM781-36B) manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-11-17 Poziotinib
1092364-38-9
US $0.00 / g 10g 98%min 1000g WUHAN FORTUNA CHEMICAL CO., LTD
2021-07-13 Poziotinib
1092364-38-9
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
2021-07-10 Poziotinib
1092364-38-9
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd

1092364-38-9(Poziotinib (HM781-36B))Related Search:


  • 1-[4-[[4-[(3,4-Dichloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-1-piperidinyl]-2-propen-1-one
  • Poziotinib
  • UNII-OEI6OOU6IK
  • 1-(4-((4-((3,4-dichloro-2-fluorophenyl)aMino)-7- Methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one
  • 1-[4-[4-(3,4-dichloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypiperidin-1-yl]prop-2-en-1-one
  • poziotinib(HM-78136B)
  • NOV120101
  • 1-[4-[[4-[(3,4-Dichloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-1-piperidinyl]-2-propen-1-one Poziotinib
  • HM781-36B)
  • Poziotinib(NOV120101
  • CS-1788
  • HM781-36B; NOV120101; NOV-120101; NOV 120101; POZIOTINIB
  • Poziotinib (HM781-37B)
  • 2-Propen-1-one, 1-[4-[[4-[(3,4-dichloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-1-piperidinyl]-
  • Poziotinib HM-781368
  • 1092364-38-9
  • C23H21Cl2FN4O3
  • Inhibitors
  • API
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