产品
编 号：F403071
分子式：C19H19N5O4S
分子量：413.45
分子式：C19H19N5O4S
分子量：413.45
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CAS No: 604769-01-9
产品详情
生物活性：
JNJ-16241199 is an orally active, selective hydroxamate-based histone deacetylase (HDAC) inhibitor, with the IC50 of 3.3 nM and 23 nM for HDAC1 and HDAC8, respectively. JNJ-16241199 induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells. JNJ-16241199 induces cell apoptosis and shows anticancer activity in a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.
体内研究：
JNJ-16241199 (每天 10-40 mpk，连续 28 天，p.o) 抑制 A2780 卵巢癌、H460 肺癌和 HCT116 结肠癌原位异种移植肿瘤模型小鼠中肿瘤的生长。Animal Model:Human A2780, H460 and HCT116 orthotopic xenograft tumor models
Dosage:10-40 mpk/day for 28 days
Administration:Oral gavage (p.o.)
Result:Induced H3 acetylation and p21waf1, cip1 promoter activity in A2780 ovarian tumour tissue. Decreased tumour volume in three orthotopic xenograft tumor models. Reached maximal decrease in final tumour volume to 76–87% in human A2780 orthotopic xenograft tumor models.
体外研究：
JNJ-16241199 对性淋巴细胞白血病 (ALL)、急性髓性白血病 (AML)、慢性淋巴细胞白血病 (CLL)、慢性髓性白血病 (CML)、淋巴瘤和骨髓瘤细胞具有抑制增殖作用 (IC50 = 15-486 nM) 。JNJ-16241199 抑制原代人乳腺上皮细胞 (HMEC) 增殖，IC50 值为 32 nM，对静止的非增殖 HMEC 细胞不敏感 (IC50 值为 7815 nM) 。JNJ-16241199 (0.1, 0.3, 1 μM, 24-48 h) 可以诱导 A2780 细胞发生细胞凋亡，并抑制其血管生成。
JNJ-16241199 is an orally active, selective hydroxamate-based histone deacetylase (HDAC) inhibitor, with the IC50 of 3.3 nM and 23 nM for HDAC1 and HDAC8, respectively. JNJ-16241199 induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells. JNJ-16241199 induces cell apoptosis and shows anticancer activity in a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.
体内研究：
JNJ-16241199 (每天 10-40 mpk，连续 28 天，p.o) 抑制 A2780 卵巢癌、H460 肺癌和 HCT116 结肠癌原位异种移植肿瘤模型小鼠中肿瘤的生长。Animal Model:Human A2780, H460 and HCT116 orthotopic xenograft tumor models
Dosage:10-40 mpk/day for 28 days
Administration:Oral gavage (p.o.)
Result:Induced H3 acetylation and p21waf1, cip1 promoter activity in A2780 ovarian tumour tissue. Decreased tumour volume in three orthotopic xenograft tumor models. Reached maximal decrease in final tumour volume to 76–87% in human A2780 orthotopic xenograft tumor models.
体外研究：
JNJ-16241199 对性淋巴细胞白血病 (ALL)、急性髓性白血病 (AML)、慢性淋巴细胞白血病 (CLL)、慢性髓性白血病 (CML)、淋巴瘤和骨髓瘤细胞具有抑制增殖作用 (IC50 = 15-486 nM) 。JNJ-16241199 抑制原代人乳腺上皮细胞 (HMEC) 增殖，IC50 值为 32 nM，对静止的非增殖 HMEC 细胞不敏感 (IC50 值为 7815 nM) 。JNJ-16241199 (0.1, 0.3, 1 μM, 24-48 h) 可以诱导 A2780 细胞发生细胞凋亡，并抑制其血管生成。
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