RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.
CAS 1041469-97-9 MFCD141469979
化学结构图
SMILES: CC1CS(=O)(=O)CCN1/N=C/c1c(Cl)c2cc(Br)ccc2oc1=O
化学属性
| Mol. Weight | 433.7 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO |
别名和识别编码
| Chemical Name | RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment. |
|---|---|
| Formula | C15H14BrClN2O4S |
| Synonym | RKS262; RKS 262; RKS-262 |
| IUPAC Name | (E)-6-bromo-4-chloro-3-(((3-methyl-1,1-dioxidothiomorpholino)imino)methyl)-2H-chromen-2-one |
| InChIKey | RPUHUUBAOXLODQ-CNHKJKLMSA-N |
| InChI | InChI=1S/C15H14BrClN2O4S/c1-9-8-24(21,22)5-4-19(9)18-7-12-14(17)11-6-10(16)2-3-13(11)23-15(12)20/h2-3,6-7,9H,4-5,8H2,1H3/b18-7+ |
| Canonical SMILES | O=C1C(/C=N/N(CC2)C(C)CS2(=O)=O)=C(Cl)C3=C(O1)C=CC(Br)=C3 |
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- RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.
