产品
编 号：F741251
分子式：C16H14N6O2
分子量：322.32
分子式：C16H14N6O2
分子量：322.32
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1636894-46-6
产品详情
生物活性：
KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models.
体内研究：
KA2507 (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model.KA2507 also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models.Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 administration resulting in reduced STAT3 activation (as measured by phospho-STAT3, an important suppressor of the antitumor immune response), reduced PD-L1 expression, and increased expression of MHC class I.KA2507 exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg).Animal Model:Male C57BL/6 mice, B16-F10 melanoma model
Dosage:100 mg/kg, 200 mg/kg, 200 mg/kg
Administration:Oral gavage, daily, for 20 days
Result:Demonstrated antitumor efficacy.
Animal Model:Male C57BL/6 mice
Dosage:200 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:Oral bioavailability (15%), Cmax (300 ng/mL).
体外研究：
KA2507 did not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition.
KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models.
体内研究：
KA2507 (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model.KA2507 also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models.Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 administration resulting in reduced STAT3 activation (as measured by phospho-STAT3, an important suppressor of the antitumor immune response), reduced PD-L1 expression, and increased expression of MHC class I.KA2507 exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg).Animal Model:Male C57BL/6 mice, B16-F10 melanoma model
Dosage:100 mg/kg, 200 mg/kg, 200 mg/kg
Administration:Oral gavage, daily, for 20 days
Result:Demonstrated antitumor efficacy.
Animal Model:Male C57BL/6 mice
Dosage:200 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:Oral bioavailability (15%), Cmax (300 ng/mL).
体外研究：
KA2507 did not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition.
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