| Identification | Back Directory | [Name]
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- | [CAS]
2563855-03-6 | [Synonyms]
N-[3-(4-Chlorophenoxy)-4-methylphenyl]acrylamide
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- | [Molecular Formula]
C16H14ClNO2 | [MDL Number]
MFCD34179527 | [MOL File]
2563855-03-6.mol | [Molecular Weight]
287.74 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. |
| [storage]
Store at -20°C, protect from light | [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. |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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