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Pictilisib dimethanesulfonate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pictilisib dimethanesulfonate图片
CAS NO:957054-33-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品名称
GDC-0941 dimethanesulfonate
GDC-0941 2 MeSO3H salt
产品介绍
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) 是一种有效的PI3Kα/δ抑制剂,IC50值为 3 nM;对 p110β 和 p110γ具有适度的选择性。
生物活性

Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor ofPI3Kα/δwithIC50of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

IC50& Target

p110α

3 nM (IC50)

p110β

33 nM (IC50)

p110δ

3 nM (IC50)

p110γ

75 nM (IC50)

p110α-H1047R

3 nM (IC50)

p110α-E545K

3 nM (IC50)

DNA-PK

1.23 μM (IC50)

mTOR

0.58 μM (Ki)

Autophagy

 

体外研究
(In Vitro)

Pictilisib (GDC-0941) 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[1]. 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. 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) than A549 cells with wild-type PIK3CA[3]. 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[4].

体内研究
(In Vivo)

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[1]. Tumours in the Pictilisib (GDC-0941)-treated mice show a marked non-linear shrinkage, and when the Pictilisib (GDC-0941) treatment ceased, the tumours in the test cohort mice grow again[2]. 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[4].

Clinical Trial
分子量

705.85

性状

Solid

Formula

C25H35N7O9S4

CAS 号

957054-33-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 7.14 mg/mL(10.12 mM;ultrasonic and warming and heat to 60℃)

DMSO : 7.14 mg/mL(10.12 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.4167 mL7.0837 mL14.1673 mL
5 mM0.2833 mL1.4167 mL2.8335 mL
10 mM0.1417 mL0.7084 mL1.4167 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。