R306465

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ-16241199 是一种具有口服活性的选择性hydroxamate-based histone deacetylase (HDAC)抑制剂，对 HDAC 1 和 HDAC8 的IC50 分别为 3.3 nM 和 23 nM。JNJ-16241199 诱导组蛋白 3 乙酰化，并显著上调 A2780 卵巢癌细胞中 p21waf1, cip1 的表达。JNJ-16241199 诱导细胞凋亡 (cell apoptosis)，并在多种人类恶性肿瘤中显示抗癌活性。JNJ-16241199 可用于癌症研究。

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.

Cell Cycle Analysis Cell Line:Human A2780 ovarian carcinoma cells Concentration:0, 0.1, 0.3, 1 μM Incubation Time:24 h or 48 h Result:Decreased in S phase at 300 nM, with a parallel increase in G1 phase, but increased in the sub-G1 fraction of cells at the 1 μM after 24 h. Increased in sub-G1 phase at all active concentrations starting from 100 nM after 48 h.

Animal Model:Human A2780, H460 and HCT116 orthotopic xenograft tumor modelsDosage: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.

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Cell Cycle/DNA Damage

HDAC

HDAC | Apoptosis

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604769-01-9

413.45

C19H19N5O4S

>98% (HPLC)

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O=C(NO)C1=CN=C(N=C1)N2CCN(CC2)S(=O)(=O)C=3C=CC=4C=CC=CC4C3

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(-20℃)

With Ice Pack

≥ 2 years