10mM in DMSO ベースライン干渉を最小限に抑える必要がある、感度の高いクロマトグラフィーおよび分析ワークフロー向け。
Store at -80°C Dry ice packs + Cold packs に出荷。正確な仕様については、ロット固有の COA をご確認ください。
SDS、COA、データシート、仕様書をダウンロードできます。ロット固有の COA はロット番号検索で入手可能です。
クロマトグラフィー、有機合成、クロスカップリング反応に関する 0 件の査読済み論文で引用されています。
Information
BS-181 HCl is a highly selectiveCDK7inhibitor withIC50of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
In vitro
BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 μM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 μM, and only shows inhibition for several kinases from other classes at high concentrations (>10 μM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 μM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.
In vivo
BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentration ~50 μM
Incubation Time：24 hours
Powder Purity:≥99%
危険性、取扱い、保管、および規制遵守を網羅した包括的な文書。
<<<<<<< HEAD SDS をダウンロード → ======= SDS をダウンロード → >>>>>>> release248-p3| 溶解度 | Solubility (25°C) In vitro DMSO: 63 mg/mL (199.49 mM); Water: 63 mg/mL (199.49 mM); Ethanol: 1 mg/mL (3.16 mM); |
|---|---|
| DMSO（mg / mL） 最大溶解度 | 83 |
| DMSO（mM） 最大溶解度 | 199.0455407 |
| 水（mg / mL） 最大溶解度 | 3 |
| 水（mM） 最大溶解度 | 7.194417132 |
