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编 号：F762920
分子式：C28H38N6O5S
分子量：570.7
分子式：C28H38N6O5S
分子量：570.7
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CAS No: 3029138-43-7
产品详情
生物活性：
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.
体内研究：
JAK/HDAC-IN-2 (化合物 21; 50 mg/kg; 腹膜内注射; 每天一次; 连续 18 天) 在体内对血液恶性肿瘤 HEL 和实体瘤 A549 中表现出有效的抗肿瘤活性。 Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats.IV (3 mg/kg) PO (15 mg/kg)
Tmax (h)2.912
Cmax (ng/mL)93.328
AUC0-t (ng/mL?h)656.241745.249
t1/2 (h)0.1282.084
CL (L/ kg?h)4.5714.56
Vss (L/kg)0.845
F (%)22.71%
Animal Model:C57BL/6 nude mice
Dosage:50 mg/kg
Administration:Intraperitoneally; once a day for 18 consecutive days
Result:Prominently reduced the weight and volume of HEL and A549 xenografts.Upgraded the expression level of acetyl-H3 as well as acetyl-tubulin and reduced the expression level of p-STAT3-Tyr705 in HEL as well as A549 xenograft tumor tissues.
体外研究：
JAK/HDAC-IN-2 (化合物 21) 对 K562、HL-60 和 HEL 细胞表现出很强的抗增殖活性 (IC50 分别为 1.87、2.26 和 0.33 μM)；抑制四种实体瘤细胞 MCF-7、HeLa、A549 和 PC-3 的增殖 (IC50 分别为 1.83、2.88、0.73 和 2.52 μM)。 JAK/HDAC-IN-2 (1, 5 μM; 24 小时) 在 HEL 细胞中具有优异的促凋亡活性，在 A549 细胞中具有中等的促凋亡活性。 JAK/HDAC-IN-2 (1, 5 μM; 24 小时) 通过抑制 HDAC 和 JAK，显着抑制血液恶性肿瘤 HEL 细胞以及实体瘤 A549 细胞中的组蛋白去乙酰化和 STAT3 磷酸化。
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.
体内研究：
JAK/HDAC-IN-2 (化合物 21; 50 mg/kg; 腹膜内注射; 每天一次; 连续 18 天) 在体内对血液恶性肿瘤 HEL 和实体瘤 A549 中表现出有效的抗肿瘤活性。 Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats.IV (3 mg/kg) PO (15 mg/kg)
Tmax (h)2.912
Cmax (ng/mL)93.328
AUC0-t (ng/mL?h)656.241745.249
t1/2 (h)0.1282.084
CL (L/ kg?h)4.5714.56
Vss (L/kg)0.845
F (%)22.71%
Animal Model:C57BL/6 nude mice
Dosage:50 mg/kg
Administration:Intraperitoneally; once a day for 18 consecutive days
Result:Prominently reduced the weight and volume of HEL and A549 xenografts.Upgraded the expression level of acetyl-H3 as well as acetyl-tubulin and reduced the expression level of p-STAT3-Tyr705 in HEL as well as A549 xenograft tumor tissues.
体外研究：
JAK/HDAC-IN-2 (化合物 21) 对 K562、HL-60 和 HEL 细胞表现出很强的抗增殖活性 (IC50 分别为 1.87、2.26 和 0.33 μM)；抑制四种实体瘤细胞 MCF-7、HeLa、A549 和 PC-3 的增殖 (IC50 分别为 1.83、2.88、0.73 和 2.52 μM)。 JAK/HDAC-IN-2 (1, 5 μM; 24 小时) 在 HEL 细胞中具有优异的促凋亡活性，在 A549 细胞中具有中等的促凋亡活性。 JAK/HDAC-IN-2 (1, 5 μM; 24 小时) 通过抑制 HDAC 和 JAK，显着抑制血液恶性肿瘤 HEL 细胞以及实体瘤 A549 细胞中的组蛋白去乙酰化和 STAT3 磷酸化。
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