Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-
PF-03814735
CAS: 942487-16-3
Molecular Formula: C23H25F3N6O2
Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]- - Names and Identifiers
Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]- - Physico-chemical Properties
| Molecular Formula | C23H25F3N6O2 |
| Molar Mass | 474.48 |
| Density | 1.443 |
| Melting Point | 181-183°C |
| Solubility | DMSO: soluble20mg/mL, clear |
| Appearance | powder |
| Color | white to beige |
| pKa | 15.02±0.46(Predicted) |
| Storage Condition | -20°C |
| In vitro study | In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2. PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells. Small cell lung cancer (SCLC) and, to a lesser extent, colon cancer lines are very sensitive to PF-03814735. The status of the Myc gene family and retinoblastoma pathway members significantly correlates with the efficacy of PF-03814735. |
| In vivo study | Once-daily oral administration of PF-03814735 to mice bearing human xenograft tumors produces a reduction in phosphohistone H3 in tumors at doses that are tolerable and that result in significant inhibition of tumor growth. The combination of PF-03814735 and docetaxel in xenograft mouse tumor models shows additive tumor growth inhibition. PF-03814735 is much more effective in NCI-H82 xenografts when administered on a weekly dosing schedule at 80 mg/kg compared with a daily schedule at 15 mg/kg. PF-03814735 delayed growth by 23.5 days on the weekly schedule, which corresponds to 0.9 logs of net cell kill during the course of treatment. |
Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]- - Risk and Safety
| WGK Germany | 3 |
Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.108 ml | 10.538 ml | 21.076 ml |
| 5 mM | 0.422 ml | 2.108 ml | 4.215 ml |
| 10 mM | 0.211 ml | 1.054 ml | 2.108 ml |
| 5 mM | 0.042 ml | 0.211 ml | 0.422 ml |
Last Update：2024-01-02 23:10:35
Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]- - Introduction
PF-03814735 is an organic compound with a chemical formula of C27H29N3O2S2 and a molecular weight of 507.66.
It is a multiple receptor tyrosine kinase inhibitor, which can act on a variety of tyrosine kinases, including EGFR, VEGFR and HER2, etc. These receptor kinases play an important role in the growth and spread of cancer cells and are therefore PF-03814735 widely studied as potential anti-cancer therapeutics.
The method of preparing PF-03814735 is relatively complicated. A common method is to synthesize them through a synthetic organic synthesis process. Specific preparation methods can be found in the specialized literature.
Pay attention to relevant safety information when using the PF-03814735. Because of its effect on tyrosine kinase, it may cause some adverse reactions during use, such as nausea, vomiting, loss of appetite, drowsiness, etc. In addition, PF-03814735 may also have certain effects on the cardiovascular system and central nervous system of the human body, so a comprehensive safety assessment is required before use. During use, it should be used in accordance with the correct dosage and method of use according to the recommendations of the doctor or professional, and pay close attention to the patient's physical response.
It is a multiple receptor tyrosine kinase inhibitor, which can act on a variety of tyrosine kinases, including EGFR, VEGFR and HER2, etc. These receptor kinases play an important role in the growth and spread of cancer cells and are therefore PF-03814735 widely studied as potential anti-cancer therapeutics.
The method of preparing PF-03814735 is relatively complicated. A common method is to synthesize them through a synthetic organic synthesis process. Specific preparation methods can be found in the specialized literature.
Pay attention to relevant safety information when using the PF-03814735. Because of its effect on tyrosine kinase, it may cause some adverse reactions during use, such as nausea, vomiting, loss of appetite, drowsiness, etc. In addition, PF-03814735 may also have certain effects on the cardiovascular system and central nervous system of the human body, so a comprehensive safety assessment is required before use. During use, it should be used in accordance with the correct dosage and method of use according to the recommendations of the doctor or professional, and pay close attention to the patient's physical response.
Last Update：2024-04-09 21:04:16
![Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-](http://res.chembk.com/assets/images/structure/312018.gif)
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Product Name: PF-03814735 Visit Supplier Webpage Request for quotation
CAS: 942487-16-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 942487-16-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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