ChemicalBook > CAS DataBase List > 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-

2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-

Product Name
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-
CAS No.
2563855-03-6
Chemical Name
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-
Synonyms
K-975, 10 mM in DMSO;N-[3-(4-Chlorophenoxy)-4-methylphenyl]acrylamide;2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-;YAP1,Cys359,pleural,TAZ,K 975,inhibit,K-975,Yes-associated protein,YAP,Inhibitor,antitumor,malignant,TEAD,K975,mesothelioma,cancer
CBNumber
CB29009022
Molecular Formula
C16H14ClNO2
Formula Weight
287.74
MOL File
2563855-03-6.mol
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2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Property

Boiling point:
442.5±45.0 °C(Predicted)
Density 
1.235±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C, protect from light
solubility 
DMSO : 220 mg/mL (764.58 mM; Need ultrasonic)
form 
Solid
pka
13.09±0.70(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML4128
Product name
K-975
Purity
≥95% (HPLC)
Packaging
1 unit
Price
$399
Updated
2025/07/31
ChemScene
Product number
CS-0158891
Product name
K-975
Packaging
25mg
Price
$650
Updated
2021/12/16
ChemScene
Product number
CS-0158891
Product name
K-975
Packaging
50mg
Price
$950
Updated
2021/12/16
ChemScene
Product number
CS-0158891
Product name
K-975
Packaging
100mg
Price
$1350
Updated
2021/12/16
ChemScene
Product number
CS-0158891
Product name
K-975
Packaging
5mg
Price
$200
Updated
2021/12/16
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2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Chemical Properties,Usage,Production

Uses

K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma[1].

Biological Activity

K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma[1]. K-975 (0.1-10000 nM; 144 h) inhibits the cell proliferation of NF2-non-expressing malignant pleural mesothelioma (MPM) cell lines[1].K-975 (10-10000 nM; 24 h) inhibits protein-protein interaction (PPI) between Halo-YAP and endogenous TEAD1/4 and Halo-TAZ and TEAD1/4 in NCI-H226 cells[1].K-975 (0.1-10000 nM; 24 h) strongly inhibits the reporter activity in NCI-H661/CTGF-Luc cells, with the maximum inhibition of ~70%, and does not inhibit the reporter activity in NCI-H661/NRF2-Luc cells[1].K-975 (1-10000 nM; 24 h) decreases the expressions of CTGF, IGFBP3, and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCI-H226 cells[1]. K-975 (10-300 mg/kg; p.o. twice a day for 14 days) inhibits the tumor growth by inhibiting YAP1/TAZ-TEAD signaling in MPM xenograft mouse models[1].

in vivo

K-975 (10-300 mg/kg; p.o. twice a day for 14 days) inhibits the tumor growth by inhibiting YAP1/TAZ-TEAD signaling in MPM xenograft mouse models[1].

Animal Model:Male SCID mice (5 weeks) injected with NCI-H226 or MSTO-211H cells[1]
Dosage:10, 30, 100, 300 mg/kg
Administration:P.o. twice a day for 14 days
Result:Exhibited strong anti-tumor effect in MPM s.c. xenograft mouse models. Decreased the expressions of CTGF, IGFBP3, and NPPB, and increased the expression of FBXO32 in the NCI-H226 xenograft model.

References

[1]. Kaneda A, et, al. The novel potent TEAD inhibitor, K-975, inhibits YAP1/TAZ-TEAD protein-protein interactions and exerts an anti-tumor effect on malignant pleural mesothelioma. Am J Cancer Res. 2020 Dec 1;10(12):4399-4415.

2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Preparation Products And Raw materials

Raw materials

Preparation Products

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2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Suppliers

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2563855-03-6, 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-Related Search:


  • 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-
  • N-[3-(4-Chlorophenoxy)-4-methylphenyl]acrylamide
  • YAP1,Cys359,pleural,TAZ,K 975,inhibit,K-975,Yes-associated protein,YAP,Inhibitor,antitumor,malignant,TEAD,K975,mesothelioma,cancer
  • K-975, 10 mM in DMSO
  • 2563855-03-6