NU223612,2759420-43-2

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NU223612

CAS No. : 2759420-43-2

MCE 国际站：NU223612

产品活性：NU223612 是一种有效的 PROTAC (PROTACs)，可降解吲哚胺 2,3-双加氧酶 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO))，K_d 为 640 nM。NU223612 通过 CRBN 介导的蛋白酶体降解有效降解 IDO1 蛋白。NU223612 以 290 nM 的亲和力与 CRBN 结合。NU223612 可以穿过血脑屏障 (BBB)。

研究领域：PROTAC  |  Metabolic Enzyme/Protease

作用靶点：PROTACs  |  Indoleamine 2,3-Dioxygenase (IDO)

In Vitro: NU223612 (0.1-10 μM; 24 h) decreases IDO1 protein levels dose-dependently.
A DC₅₀ (the concentration of the NU223612 at which 50% of the IDO1 protein is degraded) of 0.3290 μM and 0.5438 μM in U87 and GBM43 cells is determined, respectively.
NU223612 degrades IDO1 protein in multiple cell types, such as CD18 and PANC-1 human pancreatic cancer cells, OVCAR5 and SKOV3 human ovarian cancer cells, PC3 human prostate cancer cells, and the syngeneic GL261 mouse IDO1 cDNA-expressing (IDO1-O/E) glioma cell line.
NU223612 equally degrades IDO1 protein levels in both the cytoplasmic and nuclear intracellular compartments in human GBM cells. NU223612 is able to penetrate subcellular compartments.
NU223612 dose-dependently inhibits IDO1 enzyme activity resulting in decreased Kyn levels in cultured IFNγ-stimulated GBM cells. NU223612 inhibits both IDO1-mediated tryptophan metabolism as well as IDO1 non-enzyme-mediated NF-κB p65 transcription factor DNA binding activity.

In Vivo: NU223612 (25 mg/kg; i.p.; once) decreases IDO1 protein in C57BL/6 with mIDO1 cDNA-expressing GL261 cells.
NU223612 (25 mg/kg; i.p.; 5 days/week; for 3 weeks) leads to an increase in median overall survival as well as longer-term survival for up to 45 days post-tumor cell injection.
Mass spectrometry analysis of NU223612 (25 mg/kg; i.p.; once) shows a C_max of 2 μM and a half-life of 8.3 h in brain tissue. In plasma, C_max is 365 μM and the half-life is 2.5 h. The binding of NU223612 to mouse brain homogenate using a 6 h equilibrium dialysis shows NU223612 to be 99.8% bound.
Half-life, AUC, and C_max of NU223612 in serum and brain samples.

	Plasma	Brain
half-lifr (h)	2.5	8.3
AUC0-24 (μM▪h)	582	7
Cmax (μM)	365	2

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