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Narmafotinib

Product NameNarmafotinib
CAS1393653-34-3
MFC28H32F3N5O2
MW527.58
EINECS
MOL File1393653-34-3.mol

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

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

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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