Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 5-(4-cyclohexylphenyl)-3-[[3-(fluoromethyl)-1-azetidinyl]carbonyl]-2-(3-methyl-2-pyrazinyl)- manufacturers
- GNE-7883
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- $118.00
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2026-07-27
- CAS:2648450-42-2
- Purity: 99.38%
- Supply Ability: 10g
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| | Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 5-(4-cyclohexylphenyl)-3-[[3-(fluoromethyl)-1-azetidinyl]carbonyl]-2-(3-methyl-2-pyrazinyl)- Basic information |
| | Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 5-(4-cyclohexylphenyl)-3-[[3-(fluoromethyl)-1-azetidinyl]carbonyl]-2-(3-methyl-2-pyrazinyl)- Chemical Properties |
| Boiling point | 713.3±70.0 °C(Predicted) | | density | 1.43±0.1 g/cm3(Predicted) | | pka | 0.03±0.10(Predicted) | | form | Solid | | color | White to light yellow |
| | Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 5-(4-cyclohexylphenyl)-3-[[3-(fluoromethyl)-1-azetidinyl]carbonyl]-2-(3-methyl-2-pyrazinyl)- Usage And Synthesis |
| Uses | GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation[1][2][3]. | | in vivo | GNE-7883 (100 and 250 mg/kg; s.c.; once daily for 4 days) induces tumor growth arrest in NCI-H226 xenograft mice and tumor regression in MSTO-211H xenograft mice[1]. | Animal Model: | Mesothelioma NCIH226 xenograft mouse model[3] | | Dosage: | 250 mg/kg | | Administration: | Subcutaneous injection (s.c.); Once a day for 4 days | | Result: | Had a strong inhibitory effect on tumor growth in vivo, with an inhibition rate of 102%. |
| | IC 50 | YAP/TAZ-TEAD | | References | [1] Hagenbeek TJ, et al. An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance. Nat Cancer. 2023 Jun;4(6):812-828. DOI:10.1038/s43018-023-00577-0
[2] McGee L E. YAP Signaling Promotes Resistance to MEK Inhibition in NF1-Related MPNSTs[M]. Van Andel Research Institute, 2023.
[3] Barry E R, et al. Recent therapeutic approaches to modulate the Hippo pathway in oncology and regenerative medicine[J]. Cells, 2021, 10(10): 2715. DOI:10.3390/cells10102715 |
| | Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 5-(4-cyclohexylphenyl)-3-[[3-(fluoromethyl)-1-azetidinyl]carbonyl]-2-(3-methyl-2-pyrazinyl)- Preparation Products And Raw materials |
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