基本属性 生物活性体外研究体内研究 用途与合成方法 供应商 相关产品
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[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮

基本属性 生物活性体外研究体内研究 用途与合成方法 供应商 相关产品
[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮
[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮 性质
  • 密度 1.49
[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮 用途与合成方法
  • 生物活性R547是一种有效的,ATP竞争性CDK1/2/4抑制剂,Ki为2 nM/3 nM/1 nM,对CDK7和GSK3α/β作用效果稍弱,而抑制其他激酶活性。Phase 1。
  • 体外研究R547 identified as a diaminopyrimidine compound, which is a potent and selective ATP-competitive CDK inhibitor. R547 effectively inhibits CDK1/cyclinB, CDK2/cyclinE, and CDK4/cyclinD1(Ki=1-3nM) and is inactive(Ki>5,000nM) against a panel of >120 unrelated kinases. R547 effectively inhibits the proliferation of tumor cell lines independent of multidrug resistant status, histologic type, retinoblastoma protein, or p53 status, with IC50s <0.60 μM. R547 reduces phosphorylation of the cellular retinoblastoma protein at specific CDK phosphorylation sites at the same concentrations that induced cell cycle arrest, suggesting a potential pharmaco dynamics marker for clinical use. R547 inhibits the proliferation of tumor cell lines and is active in all 19 cell lines tested irrespective of tissue of origin, multidrug resistance (MDR), p53, or retinoblastoma status. R547 possessing both 5-and 6-fluoro substitution culminated in an Inhibitor with low, single-digit nanomolar potency against the CDKs(Ki=0.001,0.003,and 0.001 μM for CDK1,CDK2, and CDK4,respectively) and excellent cellular potency (IC50=0.08 μM,HCT116 cell line).
  • 体内研究R547 administered with oral and i.v. dosing in multiple established human tumor significantly inhibits tumor activity(P < 0.01). R547 administered orally at dose of 40 mg/kg daily in colon, lung, breast, prostate, and melanoma human tumor xenograft models shows significant TGI (79-99%). R547 is equally efficacious (TGI, 61-95%) when dosed with 40 mg/kg i.v. once weekly. These doses of R547 are not toxic and did not result in body weight loss. R547 does not show signs of overt toxicity during the course of the 3-week study and any gross pathology at necropsies done at the end of the studies. R547 inhibits tumor growth up to 95% in the HCT116 human colorectal tumor xenograft model in nude mice . R547 causes significant TGI in all of the models tested when dosed orally and i.v. at or below the maximum tolerated dose. R547 inhibits phosphorylation of retinoblastoma protein in tumors at the efficacious exposures in tumor xenograft models, providing a pharmacodynamic biomarker for clinical use. R547 reported here suggests that this is a promising molecule for evaluation in the treatment of solid tumors.
[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮供应商更多
  • 公司名称:医恩医疗系统研发(上海)有限公司 黄金产品
  • 联系电话:+86 (21) 5895-8002
  • 产品介绍: 英文名称:[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547)
    CAS:741713-40-6
    纯度:98% LC-MS 包装信息:10g, 50g, 100g, 1Kg 备注:S100005
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  • 公司名称:上海波以尔化工有限公司
  • 联系电话:86-15221043597
  • 产品介绍: 中文名称:[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮
    英文名称:4-Amino-2-(1-methylsulfonylpiperidin-4-yl)aminopyrimidin-5-yl(2,3-difluoro-6-methoxyphenyl)methanone(R 547)
    CAS:741713-40-6
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  • 公司名称:上海佰世凯化学科技有限公司
  • 联系电话:+86(0)21-20908456
  • 产品介绍: 英文名称:R547(Ro 4584820)
    CAS:741713-40-6
    备注:C14076
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  • 公司名称:Pure Chemistry Scientific Inc.
  • 联系电话:001-857-928-2050 or 1-888-588-9418
  • 产品介绍: 英文名称:Methanone;[4-aMino-2-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-5-pyriMidinyl](2;3-difluoro-6-Methoxyphenyl)-
    CAS:741713-40-6
    纯度:98% 包装信息:1g; 5g
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  • 公司名称:凯方医药科技(上海)有限公司
  • 联系电话:021-67220633 & 021-37212706
  • 产品介绍: 英文名称:[4-AMino-2-[(1-Methylsulfonylpiperidin-4-yl)aMino]pyriMidin-5-yl](2,3-difluoro-6-Methoxyphenyl)Methanone
    CAS:741713-40-6
    纯度:99% 包装信息:5KG;1KG
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"[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮"相关产品信息