Poziotinib (Synonyms: HM781-36B) |
| Catalog No.GC17916 |
A irreversible pan-HER inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1092364-38-9
Sample solution is provided at 25 µL, 10mM.
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Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 values of 3.2, 5.3 and 23.5 nM for HER1, HER2 and HER4, respectively [1].
Epidermal growth factor receptors (EGFR/HER1, HER2/ErbB2, HER3/ErbB3, HER4/ErbB4) are receptor tyrosine kinases and play important roles in cell proliferation and differentiation. The EGFR family is a major target of anticancer drugs [1].
Poziotinib is an irreversible pan-HER inhibitor. In HER2 amplified SNU216 and N87 gastric cancer cells, HM781-36B inhibited cell growth with IC50 values of 4 and 1 nM, respectively. Also, HM781-36B potently inhibited the phosphorylation of HER family and downstream proteins such as STAT3, AKT and ERK, and induced G1 arrest and apoptosis. HM781-36B dose-dependently increased the amount of cleaved form of effector caspases (caspase-3 and caspase-7) and PARP, reduced antiapoptotic proteins BCL-2 and MCL-1, and induced proapoptotic protein BIM [1]. In HER2-amplified breast cancer cells, HM781-36B inhibited cell growth with IC50 values of 1, 1.2 and 9.5 nM for SK-BR-3, BT474, and MDA-MB-453 cells, respectively [2].
In nude mouse bearing N87 human gastric cancer xenograft model, HM781-36B significantly inhibited tumor growth and exhibited a synergistic effect when administered with chemotherapeutic agents [1].
References:
[1]. Nam HJ, Kim HP, Yoon YK, et al. Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer. Cancer Lett, 2011, 302(2): 155-165.
[2]. Kim HJ, Kim HP, Yoon YK, et al. Antitumor activity of HM781-36B, a pan-HER tyrosine kinase inhibitor, in HER2-amplified breast cancer cells. Anticancer Drugs, 2012, 23(3): 288-297.
| Cas No. | 1092364-38-9 | SDF | |
| Synonyms | HM781-36B | ||
| Chemical Name | 1-(4-((4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one | ||
| Canonical SMILES | C=CC(N1CCC(OC2=C(OC)C=C3C(C(NC4=C(F)C(Cl)=C(Cl)C=C4)=NC=N3)=C2)CC1)=O | ||
| Formula | C23H21Cl2FN4O3 | M.Wt | 491.34 |
| Solubility | ≥ 94.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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