pf-5274857
更新时间：2023-04-02 19:49:50
采购访问：31次
| 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 | CAS号 | 1373615-35-0 |
|---|---|---|---|
| 价格 | $需询单/100g $需询单/1kg $需询单/100kg $需询单/1000kg | 纯度 | 98.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情（用途，包装等）
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 |
达阳化工（杭州）有限公司
认证状态：已认证供应商
商品数：50187件
电话：+86571-88938639
地址：浙江省杭州市西湖区文三路259号2栋9楼
地区： 浙江省 杭州市 西湖区
联系人：王小姐
联系人电话：+86-571-8893-8639
邮件：enquiry@dycnchem.com
网址：http://www.dycnchem.com
主要市场：Mainly in Southeast Asia and European and American markets
年贸易额：10 to 20 million USD
外贸占销售比例：90%
主要合作伙伴：
- 上海化源生化科技有限公司
- 上海市 上海市 普陀区
- 产品名：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
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
- 上海源溪生物科技有限公司
- 上海市 上海市 浦东新区
- 产品名：PF-5274857
- 价格： ￥需询单/1g
- 纯度：98.9%
- 备货期：1天
- 联系人：赖经理
- 上海脉铂医药科技有限公司
- 上海市 上海市 嘉定区
- 产品名：PF-5274857
- 价格： ￥3279.0/1g ￥1789.0/5mg ￥需询单/1g ￥需询单/1g
- 纯度：98.0%
- 备货期：2天
- 联系人：李先生
- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：PF-5274857
- 价格： ￥505.9/10mg ￥98.9/1mg ￥316.9/5mg ￥2753.9/100mg
- 纯度：98.0%
- 备货期：1天
- 联系人：阿拉丁
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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-丙酮生产厂家
参考价格：$216/5mg