产品
编 号：F762388
分子式：C28H24FN7O2
分子量：509.53
分子式：C28H24FN7O2
分子量：509.53
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2406278-81-5
产品详情
生物活性：
OM-153 is a potent and orally active tankyrase inhibitor with IC50s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 (TNKS1/2), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM.
体内研究：
OM-153 (0.1-10 mg/kg; p.o.; twice daily; for 34 days) reduces WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts.OM-153 potentiates anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model.Animal Model:CB17-SCID mice bearing COLO 320DM cells
Dosage:10 mg/kg, 3.3 mg/kg, 1 mg/kg, 0.33 mg/kg, or 0.1 mg/kg
Administration:p.o.; twice daily; for 34 days
Result:Reduced WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts.
Animal Model:C57BL/6N mice injected with B16-F10 tumors
Dosage:10 mg/kg, 1 mg/kg, and 0.1 mg/kg
Administration:p.o.; twice daily; for 20 days
Result:Potentiated anti-PD-1 immune checkpoint inhibition and antitumor effect.
体外研究：
OM-153 shows picomolar IC50 inhibition (0.63 nM) in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable absorption, distribution, metabolism, and excretion (ADME) properties, and an improved pharmacokinetic profile in mice.OM-153 decreases cell growth in COLO 320DM cells with a GI50 value of 10 nM and a GI25 value of 2.5 nM (concentrations resulting in 50% and 25% growth inhibition, respectively), while cell growth in RKO cells was insubstantially affected by the treatment.OM-153 inhibits WNT/β-catenin, YAP, and MYC signaling and shows an antiproliferative fffect in human cancer cell lines.
OM-153 is a potent and orally active tankyrase inhibitor with IC50s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 (TNKS1/2), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM.
体内研究：
OM-153 (0.1-10 mg/kg; p.o.; twice daily; for 34 days) reduces WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts.OM-153 potentiates anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model.Animal Model:CB17-SCID mice bearing COLO 320DM cells
Dosage:10 mg/kg, 3.3 mg/kg, 1 mg/kg, 0.33 mg/kg, or 0.1 mg/kg
Administration:p.o.; twice daily; for 34 days
Result:Reduced WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts.
Animal Model:C57BL/6N mice injected with B16-F10 tumors
Dosage:10 mg/kg, 1 mg/kg, and 0.1 mg/kg
Administration:p.o.; twice daily; for 20 days
Result:Potentiated anti-PD-1 immune checkpoint inhibition and antitumor effect.
体外研究：
OM-153 shows picomolar IC50 inhibition (0.63 nM) in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable absorption, distribution, metabolism, and excretion (ADME) properties, and an improved pharmacokinetic profile in mice.OM-153 decreases cell growth in COLO 320DM cells with a GI50 value of 10 nM and a GI25 value of 2.5 nM (concentrations resulting in 50% and 25% growth inhibition, respectively), while cell growth in RKO cells was insubstantially affected by the treatment.OM-153 inhibits WNT/β-catenin, YAP, and MYC signaling and shows an antiproliferative fffect in human cancer cell lines.
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