- ¥1719
- Selleck
- 进口
- S2699
- 2025年08月12日
企业认证
相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
低温
- 库存：
现货
- 供应商：
上海善然生物科技有限公司
| 产品描述 | CH5132799抑制I型PI3Ks，尤其是PI3Kα，IC50为14 nM；对PI3Kβδγ作用效果稍弱，对PIK3CA突变型细胞系敏感。Phase 1。 | |||||
|---|---|---|---|---|---|---|
| 靶点 | PI3Kα [1] | PI3Kγ [1] | PI3Kβ [1] | PI3Kδ [1] | mTOR [1] | View More |
| IC50 | 14 nM | 36 nM | 0.12 μM | 0.50 μM | 1.6 μM | |
| 体外研究 | CH5132799 selectively inhibits class I PI3Ks, PI3Kα (IC50 = 0.014 μM ), PI3Kβ (IC50 = 0.12 μM ), PI3Kδ (IC50 = 0.50 μM ), PI3Kγ (IC50 = 0.036 μM ), but shows less inhibition of class II PI3Ks, class III PI3k and mTOR and also no inhibitory activity (IC50 > 10 μM) against 26 protein kinases. CH5132799 exhibits more inhibitory activities against PI3Kα with oncogenic mutations E542K (IC50 = 6.7 nM), E545K (IC50 = 6.7 nM) and H1047R (IC50 = 5.6 nM) than wild-type PI3Kα. CH5132799 treated breast cnacer KPL-4 cells, which harbor the PIK3CA mutation, phosphorylation of Akt and its direct substrates, PRAS40 and FoxO1/3a and phosphorylation of downstream factors, including S6K, S6 and 4E-BP1, are effectively suppressed. Cancer cell lines harboring PIK3CA mutations are significantly sensitive to CH5132799 [1] In human tumor cell lines with PI3K pathway activation by mutation, CH5132799 shows potent antiproliferative activity [HCT116(CRC): IC50 = 0.20 lM, KPL-4(BC):13 IC50 = 0.032 lM, T-47D(BC): IC50 = 0.056 lM, SK-OV-3(Ovarian): IC50 = 0.12 lM]. CH5132799 effectively suppresses phosphorylation of AKT in KPL-4 cells. [2] | |||||
| 体内研究 | CH5132799 shows potent in vivo antitumor activity in several different xenograft models with PIK3CA mutations. CH5132799 overcomes mTORC1 inhibition-mediated Akt activation and regrowth of xenograft tumor by long-term everolimus administration. [1] CH5132799 as a clinical candidate that shows excellent oral bioavailability (BA) (101% in mouse), human liver microsomal stability and in vivo antitumor activity in the PC-3 xenograft model (TGI: 101% at 25 mg/kg, po, q.d. × 11 days). CH5132799 exhibits good oral BA in mouse, rat, monkey and dog (F: 54.2-101%). In a human breast cancer (KPL-4: PI3Ka H1047R) xenograft model in mice, oral treatment with CH5132799 (12.5 mg/kg, q.d.) shows strong tumor regression. The strong regression is maintained during the 6 week administration, even in the intermittent dosing schedule (q.d., 2 weeks on/1 week off; q.d., 5 days on/2 days off), suggesting that a flexible administration schedule can be applicable in the clinic. [2] | |||||
风险提示：丁香通仅作为第三方平台，为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全，合理判断，谨慎选购商品，商家和用户对交易行为负责。对于医疗器械类产品，请先查证核实企业经营资质和医疗器械产品注册证情况。
文献和实验心脏研究中常用的 AAV 血清型 天然的 AAV 血清型中，AAV1、AAV6、AAV8、AAV9、AAVrh.10 和 AAVrh.74 对心脏有较好的感染效率，其中： 小鼠静脉或心肌注射：AAV9 > AAV8 > AAV6 > AAV1 > AAV2（图 3-5） 大动物心肌注射：AAV6 ≥ AAV1 > AAV9（图 6） 小鼠体内：AAV9 > AAVrh.74 ≥ AAVrh.10（图 7） 图 3. 五种 AAV 血清型在小鼠体内的心脏基因递送效率比较。注射方式为颈
三句话读懂一篇 CNS，NEJM 报道首次发现癌症母婴传播；基因治疗屡获突破；绘制哺乳动物祖先的基因图谱...
发表论文 A noninflammatory mRNA vaccine for treatment of experimental autoimmune encephalomyelitis，研究人员合成 了类似新冠疫苗、不引发免疫反应的 mRNA 疫苗，通过驯化调节性 T 细胞，引发免疫耐受，成功治疗小鼠实验性自身免疫性脑脊髓炎，该工作为后续的临床治疗指明了方向。 图 7. 来源于 Science 8. Cell: 细菌内源 sgRNA 利用 Cas9 下调 CRISPR-Cas 系统2021 年 1 月 8 日，美国约翰・霍普金
相关专题 它们都是BSA N,O-Bis(trimethylsilyl)acetamide [BSA ] 别名：N,O-双(三甲基硅基)乙酰胺 CAS No： 10416-59-8 分子 式：C8H21NOSi2 分子量：203.43 通用名称：BSA 性状： 无色至浅黄色液体，b.p ,74-76oC,fp42oC,d420 0.829,nd20 1.417
技术资料暂无技术资料 索取技术资料
