产品
编 号：F762722
分子式：C52H54F2N7O10PS2
分子量：1070.13
分子式：C52H54F2N7O10PS2
分子量：1070.13
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规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2984506-77-4
产品详情
生物活性：
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models. AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
AK-2292 (50-200 mg/kg; i.p. once a day, 5 days a week for 3 weeks) 抑制小鼠 MV4;11 异种移植模型中的肿瘤生长。AK-2292 (150 mg/kg; a single i.p.) 诱导小鼠 MV4;11 异种移植组织中的 STAT5 和 pSTAT5Y694 蛋白 >95% 的快速消耗。AK-2292 (i.p.) 表现出良好的血浆暴露，血浆半衰期为 1.9 h，清除率适中 (CL=0.77 L/h/kg)，体积分布良好 (Vz=2.1 L/kg)。Animal Model:SCID mice bearing MV4;11 tumors
Dosage:50, 100, 200 mg/kg
Administration:I.p. injection, once a day, 5 days per week for 3 weeks
Result:Inhibited tumor growth in a dose-dependent manner and achieved 50, 60, and 80% of tumor growth inhibition at doses of 50, 100, and 200 mg/kg, respectively.Did not induce animal weight loss or any other signs of toxicity.
体外研究：
AK-2292 (0.0015-15 μM; 4 days) 抑制 SKNO1，MV4;11 和 Kasumi-3 细胞的生长，IC50 值分别为 0.36，0.35 和 0.18 μM 。AK-2292 (0.008-5 μM; 18 h) 降低 SKNO1 细胞系中 STAT5A，STAT5B 和 pSTAT5Y694 蛋白的水平。AK-2292 (0.008-5 μM; 6 h) 有效降低 MV4;11 急性白血病细胞系中 STAT5 和 pSTAT5Y694 的水平。
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models. AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
AK-2292 (50-200 mg/kg; i.p. once a day, 5 days a week for 3 weeks) 抑制小鼠 MV4;11 异种移植模型中的肿瘤生长。AK-2292 (150 mg/kg; a single i.p.) 诱导小鼠 MV4;11 异种移植组织中的 STAT5 和 pSTAT5Y694 蛋白 >95% 的快速消耗。AK-2292 (i.p.) 表现出良好的血浆暴露，血浆半衰期为 1.9 h，清除率适中 (CL=0.77 L/h/kg)，体积分布良好 (Vz=2.1 L/kg)。Animal Model:SCID mice bearing MV4;11 tumors
Dosage:50, 100, 200 mg/kg
Administration:I.p. injection, once a day, 5 days per week for 3 weeks
Result:Inhibited tumor growth in a dose-dependent manner and achieved 50, 60, and 80% of tumor growth inhibition at doses of 50, 100, and 200 mg/kg, respectively.Did not induce animal weight loss or any other signs of toxicity.
体外研究：
AK-2292 (0.0015-15 μM; 4 days) 抑制 SKNO1，MV4;11 和 Kasumi-3 细胞的生长，IC50 值分别为 0.36，0.35 和 0.18 μM 。AK-2292 (0.008-5 μM; 18 h) 降低 SKNO1 细胞系中 STAT5A，STAT5B 和 pSTAT5Y694 蛋白的水平。AK-2292 (0.008-5 μM; 6 h) 有效降低 MV4;11 急性白血病细胞系中 STAT5 和 pSTAT5Y694 的水平。
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