1-[4-(5'-氯-3,5-二甲基[2,4'-联吡啶]-2'-基)-1-哌嗪基]-3-(甲基磺酰基)-1-丙酮

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发布时间： 2024-07-15 12:31:45

CAS号：1373615-35-0

常用名： 1-[4-(5'-氯-3,5-二甲基[2,4'-联吡啶]-2'-基)-1-哌嗪基]-3-(甲基磺酰基)-1-丙酮

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纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.IC50 value: 5.8 nMTarget: Smoothenedin vitro: PF-5274857 completely inhibits Shh-induced Hh pathway activity with IC50 of 2.7 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells. The μ-opioid receptor is weakly inhibited by PF-5274857 with a dissociation constant of 36 μM subsequently determined in a functional assay [1].in vivo: PF-5274857 shows significant dose-dependent tumor growth inhibition (TGI) and induces tumor regression at high doses(>10 mg/kg)., PF-5274857 downregulates Gli1, Gli2, Ptch1, and Ptch2 gene expression levels to various degrees with maximal effects being achieved between 6 and 12 hours post-dose (Gli1 is the most sensitive gene), whereas PF-5274857 has little effect on Smo levels. In skin tissue, downregulation of Gli1 and Gli2 is also observed with a similar time course by PF-5274857. The model-derived drug concentration for half maximal inhibition of the tumor Gli1 mRNA production rate (IC50) by PF-5274857 is determined to be 8.9 nM in the Ptch+/?p53+/? medulloblastoma allograft mice, which mathematically corresponds to tumor regression of 119% TGI after 6 days of plasma exposure at this concentration. In the Ptch+/?p53?/? medulloblastoma allograft mice, the IC50 value is estimated to be 3.5 nM, consistent with the Ptch+/?p53+/? results. PF-5274857 is also able to cross the blood–brain barrier in rats within 4 hours post-dose [1]. 物理化学性质： CAS号：1373615-35-0 常用中文名：1-[4-(5'-氯-3,5-二甲基[2,4'-联吡啶]-2'-基)-1-哌嗪基]-3-(甲基磺酰基)-1-丙酮常用英文名：PF-5274857 分子式：C20H25ClN4O3S 分子量：436.956 密度：1.3±0.1 g/cm3 沸点：686.0±55.0 °C at 760 mmHg 熔点：N/A 闪点：368.7±31.5 °C 储存条件：room temp

供应商信息：

公司名：上海念兴实业有限公司推荐

认证状态： 已认证供应商

商品数： 403768件

电话： 18916513247

地址： 2222 Huancheng Road, Juyuan New District, Jiading District, Shanghai

地区： 上海市普陀区

联系人： 小陈

联系人电话： 0086-021-52280163

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2022-02-19 价格：￥505.9 PF-5274857

2024-07-15 价格：需询单 1-[4-(5'-氯-3,5-二甲基[2,4'-联吡啶]-2'-基)-1-哌嗪基]-3-(甲基磺酰基)-1-丙酮

2022-05-12 价格：$需询单 pf-5274857

2023-10-24 价格：￥需询单 PF5274857

2021-02-06 价格：￥3279.0 PF-5274857

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1-[4-(5'-氯-3,5-二甲基[2,4'-联吡啶]-2'-基)-1-哌嗪基]-3-(甲基磺酰基)-1-丙酮价格

1-[4-(5'-氯-3,5-二甲基[2,4'-联吡啶]-2'-基)-1-哌嗪基]-3-(甲基磺酰基)-1-丙酮

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