EM-12

Name: EM-12
Brand: TargetMol
SKU: T41362
Price: 108 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.34%

货号 T41362Cas号 26581-81-7

别名 Phthalimidinoglutarimide, 2-(2,6-Dioxopiperidin-3-yl)phthalimidine

2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12 (2-(2,6-Dioxopiperidin-3-yl)phthalimidine)) 是一种致畸 Thalidomide 类似物，比 Thalidomide 活性更高，水解更稳定。2-(2,6-Dioxopiperidin-3-yl)phthalimidine 增强 1,2-dimethylhydrazine 诱导大鼠结肠癌的作用。

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EM-12

一键复制产品信息

很棒

纯度: 99.34%

货号 T41362 别名 Phthalimidinoglutarimide, 2-(2,6-Dioxopiperidin-3-yl)phthalimidineCas号 26581-81-7

规格	价格	库存
1 mg	¥ 108	现货
5 mg	¥ 263	现货
10 mg	¥ 428	现货
25 mg	¥ 828	现货
50 mg	¥ 1,180	现货
100 mg	¥ 1,820	现货
200 mg	¥ 2,590	现货
1 mL x 10 mM (in DMSO)	¥ 288	现货

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产品介绍

EM-12 AI Summary

EM-12 displays significant bioactivity and pharmacokinetic properties across a range of assays. Notably, it inhibits angiogenesis in a rat aortic ring model, exhibiting a consistent 30% inhibition of microvessel outgrowth at concentrations of 100 uM and 200 uM in Endothelial Basal Medium with Dimethylsulfoxide. The compound demonstrates favorable distribution characteristics, with a logD value of 0.498 at 1 mg/ml under pH 7.4 conditions and good permeability in human Caco-2 cells, with an apparent permeability of 22.2 x 10^-6 cm/s and an efflux ratio close to 1 (0.99). It also has high kinetic solubility in PBS at 200 uM, with solubility reaching 451,000 nM after 30 minutes of incubation. In terms of metabolic stability, EM-12 exhibits a half-life of 1.983 hours in human plasma and greater than 3.1 hours in human liver microsomes in the presence of NADPH. The compound shows relatively low intrinsic clearance rates in both human liver microsomes and hepatocytes, indicating higher metabolic stability. Within human MOLT-4 cells, EM-12 achieves complete drug accumulation and maintains a high intracellular bioavailability of 220.0%. The compound also modulates CRBN/IKZF1, demonstrating Protac activity with a DC50 value of 192.7 nM and 69.0% maximum degradation of IKZF1 after 24 hours. Overall, EM-12 offers substantial therapeutic potential due to its robust bioactivity, favorable distribution, and metabolic profiles..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12 (2-(2,6-Dioxopiperidin-3-yl)phthalimidine)) is a teratogenic Thalidomide analogue that is more active than Thalidomide and is much more stable for hydrolysis. 2-(2,6-Dioxopiperidin-3-yl)phthalimidine enhances 1,2-dimethylhydrazine-induction of rat colon adenocarcinomas [1] [2].
别名	Phthalimidinoglutarimide, 2-(2,6-Dioxopiperidin-3-yl)phthalimidine

化学信息

分子量	244.25
分子式	C₁₃H₁₂N₂O₃
CAS No.	26581-81-7
Smiles	O=C1N(CC=2C1=CC=CC2)C3C(=O)NC(=O)CC3
密度	1.2650 g/cm3 (Estimated)
颜色	Blue
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 11 mg/mL (45.04 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	4.0942 mL	20.4708 mL	40.9417 mL	204.7083 mL
5 mM	0.8188 mL	4.0942 mL	8.1883 mL	40.9417 mL
10 mM	0.4094 mL	2.0471 mL	4.0942 mL	20.4708 mL
20 mM	0.2047 mL	1.0235 mL	2.0471 mL	10.2354 mL