PARP7-IN-14
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 534.46 |
| Molecular Formula | C21H24F6N8O2 |
| SMILES | O=C1NN=CC(N[C@H](CN2CC(C(N3CCN(CC3)C4=NC=C(C=N4)C(F)(F)F)=O)C2)C)=C1C(F)(F)F |
Summary
In Vitro
PARP7-IN-14 (I-1) inhibits CT26 cell lines with the IC
50
value of 12.85 μM and shows some anti-proliferative effect on tumors
[1]
.
PARP7-IN-14 (I-1) (0-4 μM) promotes mRNA expression levels of IFN-β and CXCL10 and induces a concentration-dependent increase in STAT1 phosphorylation in CT26 cell lines
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PARP7-IN-14 (I-1) (p.o., 25-100 mg/kg, twice daily, 14 days) significantly inhibits tumour growth in CT26 tumour-bearing mice, with a 67% reduction in mean tumour volume in mice treated with I-1 compared to controls, and does not cause weight loss or other signs of toxicity
[1]
.
The pharmacokinetic parameters of PARP7-IN-14 (I-1) in ICR mice
| Parameters | T 1/2 (h) | T max (h) | C max (g/mL) | C 0 (ng/mL) | AUC 0-∞ (h*ng/mL) | V z (mL/kg) | CL (mL/h/kg) | MRT 0-∞ (h) | F (%) |
| IV (1 mg/kg) | 1.44 | 0.08 | 418.6 | 503.9 | 591.1 | 3659.3 | 1741.4 | 1.68 | - |
| PO (10 mg/kg) | 1.74 | 0.58 | 2300 | - | 5663.5 | 4583.6 | 1816.0 | 1.97 | 95.8 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.