RRD-251盐酸盐是Rb / Raf-1相互作用的可逆，有效和选择性破坏剂。视网膜母细胞瘤抑癌蛋白（Rb）通过抑制E2F转录因子家族的转录活性来控制G1-S边界。Raf-1激酶在G1期早期与Rb结合并使其磷酸化。RRD-251在体内以Rb依赖性方式显着抑制血管生成和肿瘤生长。RRD-251不会抑制B-Raf与Rb的结合以及Raf-1与Mek1 / 2的结合。同样，RRD-251不会影响与细胞周期蛋白D，细胞周期蛋白E或Raf-1相关的激酶活性。 RRD-251 hydrochloride is a reversible, potent, and selective disruptor of Rb/Raf-1 interaction. The retinoblastoma tumor suppressor protein (Rb) controls the G1-S boundary by repressing the transcriptional activity of the E2F family of transcription factors. Raf-1 kinase binds and phosphorylates Rb early in the G1 phase. RRD-251 significantly inhibits angiogenesis and tumor growth in vivo in an Rb-dependent manner. RRD-251 does not inhibit the binding of B-Raf to Rb and Raf-1 to Mek1/2. Also, RRD-251 does not affect the kinase activities associated with cyclin D, cyclin E, or Raf-1.
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RRD-251 hydrochloride
Dangerous GoodsCAS number：72214-67-6 molecular formula：C8H8Cl2N2S· HCl
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 2,4-dichlorobenzyl imidothiocarbamate hydrochloride | (2,4-Dichlorophenyl)carbamimidothioic acid methyl ester hydrochloride | 2-(2,4-Dichlorobenzyl)-2-thiopseudourea hydrochloride | Rb/Raf-1 disruptor 251 hydrochloride | S-(2,4-Dichlorobenzyl)-isothiouron | ||
| CAS number | 72214-67-6 | molecular formula | C8H8Cl2N2S· HCl |
| molecular weight | 271.59 g/mol | Exact mass | ≥98% |
| PSA | 75.200 Ų | logp | - |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P270: 使用本产品时，请勿进食、饮水
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