Pictilisib dimethanesulfonate
作者：齐岳
发布时间：2023-09-13
17:32:17
点击数：
产品名称：Pictilisib dimethanesulfonate
产品描述：
| 产品描述 | Pictilisib dimethanesulfonate is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). |
| 靶点活性 | p110γ:75 nM, p110β:33 nM, p110α:3 nM, p110α-H1047R:3 nM, p110α-E545K:3 nM, p110δ:3 nM, mTOR:0.58 μM (Ki), DNA-PK:1.23 μM |
| 体外活性 | Pictilisib (GDC-0941) is highly efficacious in combination with U0126 in inducing cell growth inhibition, G0-G1 arrest and cell apoptosis. H460 cells with activating mutations of PIK3CA are relatively more sensitive to Pictilisib (GDC-0941) compared to A549 cells with wild-type PIK3CA. Pictilisib (GDC-0941) reduces PI3K pathway activity in both cell lines, illustrated by decreased pAK. Pictilisib (GDC-0941) significantly reduces secreted VEGF detected in the medium after hypoxic/anoxic exposure in all cells. Pictilisib and RP-56976 reduce tumor cell viability by 80% or greater in the breast cancer cell lines than single-agent treatment. GDC-0941 inhibits Akt phosphorylation and downstream targets of Akt signaling such as pPRAS40 and pS6 in Hs578T1.2 (PI3Kα wild-type), MCF7-neo/HER2 (PI3Kα-mutant), and MX-1 (PTEN-null) tumor models. Pictilisib (GDC-0941) decreases the time of RP-56976-induced mitotic arrest prior to apoptosis. Pictilisib (GDC-0941) shows a high efficacy of antitumor activity in two ZD1839-resistant non-small cell lung cancer (NSCLC) cell lines, A549 and H460. |
| 体内活性 | Tumours in the Pictilisib (GDC-0941)-treated mice exhibit a significant non-linear shrinkage, and when the Pictilisib (GDC-0941) treatment ceased, the tumours in the test cohort mice grow again. GDC-0941Pictilisib (GDC-0941) (25 or 50 mg/kg) reduces tumor growth and PI3K and HIF-1 pathway activity in eGFP-FTC133 tumor-bearing mice.Pictilisib (GDC-0941) (150 mg/kg, p.o.) leads to tumor stasis in MCF7-neo/HER2-bearing animals model. Pictilisib (GDC-0941) and RP-56976 result in tumor regressions during the treatment period leading to enhanced antitumor responses. |
| 别名 | GDC-0941 2 MeSO3H salt, GDC-0941 dimethanesulfonate |
| 分子量 | 705.85 |
| 分子式 | C25H35N7O9S4 |
| CAS No. | 957054-33-0 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 50 mg/mL (70.84 mM),Need ultrasonic
H2O: < 0.1 mg/mL (insoluble)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
