ETP-46321

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ETP-46321

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。

CAS NO:

1252594-99-2

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

ETP-46321 是一种有效的PI3Kα和PI3Kδ抑制剂，K_iapp分别为 2.3 和 14.2 nM。

生物活性

ETP-46321 is a potent and orally bioavailablePI3KαandPI3Kδinhibitor withK_iapps of 2.3 and 14.2 nM, respectively.

IC₅₀& Target^[1]

p110α

2.3 nM (Ki)

PI3Kα-E545K

1.77 nM (Ki)

PI3Kα-E542K

1.89 nM (Ki)

PI3Kα-H1047R

2.33 nM (Ki)

p110δ

14.2 nM (Ki)

p110β

170 nM (Ki)

p110γ

179 nM (Ki)

体外研究
(In Vitro)

ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (K_iapp=2.3 nM). ETP-4632, has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K and H1047R), being equipotent against these mutants when compared to the wild type protein (K_iapp=2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorilation of AKT in U2OS cell line with an IC₅₀of 8.3 nM^[1].

体内研究
(In Vivo)

ETP-46321, is selected for in vivo studies based on its appealing pharmacokinetic profile in BALB-C mice, low in vivo Clearance (0.6 L/h/Kg) and good oral bioavailability (90%). ETP-46321 demonstrates a good pharmacokinetic profile in mice and is selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation, showing significant tumor growth inhibition, and reduction of the tumor metabolic activity as measured by positron emission tomography (PET) techniques^[1].

分子量

473.55

性状

Solid

Formula

C₂₀H₂₇N₉O₃S

CAS 号

1252594-99-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 33 mg/mL(69.69 mM)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.1117 mL	10.5585 mL	21.1171 mL
5 mM	0.4223 mL	2.1117 mL	4.2234 mL
10 mM	0.2112 mL	1.0559 mL	2.1117 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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。