CHK1-IN-9
CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026).
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- Formule: C19H18F2N8O
- Masse moléculaire:412.40
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Activité biologique
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Chk1 0.55 nM (IC50) |
CHK1-IN-9 (compound 11) (11.11, 33.33, 100, and 300 nM, 16 h) can inhibit the proliferation of tumor cells, with the IC50 value of 202 nM for MV-4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OVCAR3, HT-29, A549, HL-60, HCT116, A2780 and MDAMB-468 cells
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Concentration:11.11, 33.33, 100, and 300 nM
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Incubation Time:16 h
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Result:Alone had an IC50 value of 1166.5 nM for HT-29, and 63.53 nM when combined with Gemcitabine (HY-17026).
Pharmacokinetic Analysis in the HT-29 xenograft mouse model Model[1]
| Route | Dose (mg/kg) | C0 (ng/mL) | Cmax (ng/mL) | T1/2 (h) | Tmax (h) | AUC0-t (ng·h/mL) | AUC0-∞ (ng·h/mL) | MRT0-t (h) | MRT0-t (h) | Cl (mL/kg/min) | Vss (L/kg) | F (%) |
| i.v. | 2 | 860 | 526 | 5.70 | 0.08 | 327 | 341 | 2.67 | 3.91 | 98.4 | 23.3 | / |
| p.o. | 10 | / | 81.1 | 1.51 | 0.08 | 40.7 | 47.3 | 1.00 | 1.65 | / | / | 2.77 |