| Identification | Back Directory | [Name]
1-Piperazinecarboxamide, N-[4-[[1,6-dihydro-6-oxo-5-(trifluoromethyl)-4-pyridazinyl]amino]butyl]-4-[5-(trifluoromethyl)-2-pyrimidinyl]- | [CAS]
2946705-91-3 | [Synonyms]
1-Piperazinecarboxamide, N-[4-[[1,6-dihydro-6-oxo-5-(trifluoromethyl)-4-pyridazinyl]amino]butyl]-4-[5-(trifluoromethyl)-2-pyrimidinyl]- | [Molecular Formula]
C19H22F6N8O2 | [MOL File]
2946705-91-3.mol | [Molecular Weight]
508.42 |
| Hazard Information | Back Directory | [Uses]
PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy[1]. | [in vivo]
PARP7-IN-22 (XLY-1) (Male rats, 5 mg/kg, i.v.; 30 mg/kg, p.o; 0.5-24 h) can be administered orally for further in vivo pharmacodynamic studies[1].PARP7-IN-22 (CT26 syngeneic model, 25 or 50 mg/kg, p.o., 14 days) demonstrates excellent anti-tumor proliferative effects in the CT26 syngeneic model [1].PARP7-IN-22 (CT26 syngeneic model, 50 mg/kg, p.o., 14 days) promotes T cell infiltration into tumor tissues and exhibits targeted effects[1]. 1.19 Pharmacokinetic Analysis in CT26 Syngeneic Model[1]|
| PARP7-IN-22 (XLY-1) | T1/2 (h) | Tmax (h) | Cmax(g/mL) | C0(g/mL) | AUC0-∞ (h ng/mL) | Vz (L/kg) | CL (L/h/kg) | MRT0-∞(h) | F (%) | | i.v. (5 mg/kg) | 5.42 | 1.25 | 353.80 | 1632.80 | 1626.00 | 0.029 | 0.004 | 3.22 | - | | p.o. (30 mg/kg) | 5.52 | 1.75 | 674.00 | - | 2368.10 | 0.112 | 0.014 | 4.84 | 24.27 |
| [IC 50]
PARP-7: 0.6 nM (IC50) | [References]
[1] Yang J, et al. Discovery of highly potent PARP7 inhibitors for cancer immunotherapy[J]. Bioorganic Chemistry, 2024, 148: 107469. DOI:10.1016/j.bioorg.2024.107469 |
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