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Narmafotinib

Product Name
Narmafotinib
CAS No.
1393653-34-3
Chemical Name
Narmafotinib
Synonyms
AMP-945;CTx-0294945;Narmafotinib;Unii-16T7U12J7U;AMP-945, 10 mM in DMSO;Focal adhesion kinase,Inhibitor,PTK2 protein tyrosine kinase 2,inhibit,AMP945,PTK2,AMP-945,AMP 945,FAK;2-(2-(2-(2-((2-Methoxy-4-(1-methylpiperidin-4-yl)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)ethyl)phenyl)acetamide;Benzeneacetamide, 2-[2-[2-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]ethyl]-
CBNumber
CB78246546
Molecular Formula
C28H32F3N5O2
Formula Weight
527.58
MOL File
1393653-34-3.mol
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Narmafotinib Property

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
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Hazard and Precautionary Statements (GHS)

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Narmafotinib Chemical Properties,Usage,Production

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.

Narmafotinib Preparation Products And Raw materials

Raw materials

Preparation Products

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Narmafotinib Suppliers

China 30 United States 3 Global 33
BOC Sciences
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1-631-485-4226; 16314854226
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info@bocsci.com
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United States
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ShangHai Biochempartner Co.,Ltd
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177-54423994 17754423994
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QQ:2853530913
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2853530910@QQ.com
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Shanghai Chaolan Chemical Technology Center
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021-QQ：65489617 15618227136
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21-5161 9052
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Sales@ATKchemical.com
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Fujian boshi pharmaceutical technology co. LTD
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0595-22008920; 18120708884
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393612455@qq.com
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Suzhou Chenrui Biotechnology Co. LTD
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17625585511
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qq：1580084073
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Chunchuang (Wuhan) Technology Co., Ltd
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15727060112
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yutianchun2007@126.com
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China
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Hangzhou Taorui Biotechnology Co., Ltd
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4000-360-990 15268198094
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sales@torreybio.com
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China
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Hebei Weite Medical Technology Co., Ltd
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13180081292 13180081292
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contact@wetogethermed.com
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Zhengzhou convergence chemical co., LTD
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0371-0371-55153829 18003835034
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Hubei wei shi reagent group ltd., company
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027-59102966 18717199209
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1393653-34-3, NarmafotinibRelated Search:

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  • 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
  • 1393653-34-3
  • C28H32F3N5O2