R306465, also known as JNJ-16241199, is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models. R306465 was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro. R306465 potently inhibited cell proliferation of all main solid tumour indications, including ovarian, lung, colon, breast and prostate cancer cell lines, with IC50 values ranging from 30 to 300 nM. The high activity of R306465 in cell-based assays and in vivo after oral administration makes R306465 a promising novel antitumoral agent with potential applicability in a broad spectrum of human malignancies. N-羟基-2-[4-(2-萘基磺酰基)-1-哌嗪基]-5-嘧啶甲酰胺
CAS 604769-01-9 MFCD04769019
化学结构图
SMILES: O=C(NO)c1cnc(N2CCN(S(=O)(=O)c3ccc4ccccc4c3)CC2)nc1
化学属性
| Mol. Formula | C19H19N5O4S |
|---|---|
| Mol. Weight | 413.45026 |
| Appearance | Solid powder |
| Solubility | Soluble in DMSO |
别名和识别编码
| Chemical Name | R306465, also known as JNJ-16241199, is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models. R306465 was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro. R306465 potently inhibited cell proliferation of all main solid tumour indications, including ovarian, lung, colon, breast and prostate cancer cell lines, with IC50 values ranging from 30 to 300 nM. The high activity of R306465 in cell-based assays and in vivo after oral administration makes R306465 a promising novel antitumoral agent with potential applicability in a broad spectrum of human malignancies. |
|---|---|
| Chemical Name Translation | N-羟基-2-[4-(2-萘基磺酰基)-1-哌嗪基]-5-嘧啶甲酰胺 |
| Chemicalbook ID | CB7950388 |
| Formula | C19H19N5O4S |
| Synonym | R 306465; R306465; R-306465; JNJ16241199; JNJ-16241199; JNJ 16241199. |
| IUPAC Name | N-hydroxy-2-(4-(naphthalen-2-ylsulfonyl)piperazin-1-yl)pyrimidine-5-carboxamide |
| InChIKey | MUTBJZVSRNUIHA-UHFFFAOYSA-N |
| InChI | InChI=1S/C19H19N5O4S/c25-18(22-26)16-12-20-19(21-13-16)23-7-9-24(10-8-23)29(27,28)17-6-5-14-3-1-2-4-15(14)11-17/h1-6,11-13,26H,7-10H2,(H,22,25) |
| Canonical SMILES | O=C(C1=CN=C(N2CCN(S(=O)(C3=CC=C4C=CC=CC4=C3)=O)CC2)N=C1)NO |
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- R306465, also known as JNJ-16241199, is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models. R306465 was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro. R306465 potently inhibited cell proliferation of all main solid tumour indications, including ovarian, lung, colon, breast and prostate cancer cell lines, with IC50 values ranging from 30 to 300 nM. The high activity of R306465 in cell-based assays and in vivo after oral administration makes R306465 a promising novel antitumoral agent with potential applicability in a broad spectrum of human malignancies.
