Narmafotinib
Narmafotinib Basic information
- Product Name:
- Narmafotinib
- Synonyms:
-
- Benzeneacetamide, 2-[2-[2-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]ethyl]-
- AMP-945
- Focal adhesion kinase,Inhibitor,PTK2 protein tyrosine kinase 2,inhibit,AMP945,PTK2,AMP-945,AMP 945,FAK
- Unii-16T7U12J7U
- Narmafotinib
- 2-(2-(2-(2-((2-Methoxy-4-(1-methylpiperidin-4-yl)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)ethyl)phenyl)acetamide
- AMP-945, 10 mM in DMSO
- CTx-0294945
- CAS:
- 1393653-34-3
- MF:
- C28H32F3N5O2
- MW:
- 527.58
- Mol File:
- 1393653-34-3.mol
Narmafotinib Chemical Properties
- Boiling point:
- 658.2±65.0 °C(Predicted)
- Density
- 1.259±0.06 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light
- pka
- 16.18±0.40(Predicted)
- form
- Solid
- color
- White to light yellow
Narmafotinib Usage And Synthesis
Description
NARMAFOTINIB is a small molecule drug with a maximum clinical trial phase of II and has 1 investigational indication.
Uses
Narmafotinib (AMP-945) is an orally active inhibitor of the enzyme focal adhesion kinase (FAK, KD=0.21 nM). Narmafotinib inhibits autophosphorylation of 397Y-FAK in MDA-MB-231 cells with an IC50=7 nM and exhibits low general cellular toxicity (IC50=2.7 μM, MDA-MB-231 cells). Narmafotinib can be used for anti-cancer study[1].
Biological Activity
Narmafotinib (AMP-945) is an orally active inhibitor of the enzyme focal adhesion kinase (FAK, KD=0.21 nM). Narmafotinib inhibits autophosphorylation of 397Y-FAK in MDA-MB-231 cells with an IC50=7 nM and exhibits low general cellular toxicity (IC50=2.7 μM, MDA-MB-231 cells). Narmafotinib can be used for anti-cancer study.
in vivo
Narmafotinib (80 mg/kg; p.o.; daily for 28 days) combined with Bevacizumab (HY-P9906) prevents tumor progression and enhances the durability of response in MDA-MB-231 xenograft mice model[1].
| Animal Model: | Mice were injected orthotopically with MDA-MB-231 cells[1] |
| Dosage: | 80 mg/kg |
| Administration: | Oral gavage (p.o.); daily for 28 days |
| Result: | Tumor growth was significantly inhibited (88% TGI) in combination with Bevacizumab (HY-P9906) after 28 days. When the Bevacizumab treatment group tumor size reached ethical end point (1000 mm3), the average size of the tumors in the combination group was still only 562 mm3. |
References
[1] I. STREET. Abstract LB-308: Combination of CTx-0294945 a highly selective inhibitor of focal adhesion kinase with bevacizumab in pre-clinical models of breast cancer[J]. Cancer research, 2012, 11 1. DOI:10.1158/1538-7445.AM2012-LB-308.
[2] JOHN LAMBERT. Abstract CT511: A phase 1 trial of AMP945, a potent and selective focal adhesion kinase inhibitor, in healthy volunteers[J]. Cancer research, 2022. DOI:10.1158/1538-7445.am2022-ct511.
[3] COCK T A, BISHOP A, KRUGER N, et al. Abstract CT220: Phase 1b/2a of narmafotinib (AMP945) in combination with gemcitabine and nab-paclitaxel (Abraxane) standard of care as first-line therapy in patients with advanced pancreatic cancer (ACCENT trial): interim analysis[J]. ACS Chemical Health & Safety, 2024, 6 3. DOI:10.1158/1538-7445.am2024-ct220.
[4] C. BURNS. The effect of adding a selective FAK inhibitor AMP945 to FOLFIRINOX in a model of pancreatic cancer.[J]. Journal of Clinical Oncology, 2023. DOI:10.1200/jco.2023.41.16\_suppl.e15128.
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