BRD4/CK2-IN-1,2756851-99-5

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BRD4/CK2-IN-1

CAS No. : 2756851-99-5

MCE 国际站：BRD4/CK2-IN-1

产品活性：BRD4/CK2-IN-1 是一种首次高效、口服有效的 BRD4/CK2 (含溴结构域蛋白 4/酪蛋白激酶 2) 双靶点抑制剂。BRD4/CK2-IN-1 对 BRD4 和 CK2 的 IC₅₀ 值分别为 180 nM 和 230 nM。BRD4/CK2-IN-1具有很强的抗癌活性，且无明显毒性。BRD4/CK2-IN-1 在三阴性乳腺癌 (TNBC) 中诱导细胞凋亡和自噬相关的细胞死亡。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  Cell Cycle/DNA Damage  |  Apoptosis  |  Autophagy

作用靶点：Epigenetic Reader Domain  |  Casein Kinase  |  Apoptosis  |  Autophagy

In Vitro: BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect with IC₅₀s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively.
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells.
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3.
BRD4/CK2-IN-1 (0-10 μM; 24 hours) significantly downregulates the autophagy substrate p62 and up-regulated beclin-1 and LC3II in MDA-MB-231 and MDA-MB.

In Vivo: BRD4/CK2-IN-1 (25 and 50 mg/kg; intragastric administration; daily for 19 days) inhibits tumor growth in TNBC xenograft models.
BRD4/CK2-IN-1 (25 and 50mg/kg; intragastric administration; daily for 19 days) shows weak toxicity measured by body weight loss in the MDA-MB-231 and MDA-MB-468 xenograft models.
Preliminary Assessment of Pharmacokinetics (PK) profile of BRD4/CK2-IN-1.

Parameter	iv (1 mg/kg)	po (10 mg/kg)
T1/2 (h)	4.21±0.57	5.14±0.71
Cmax (ng/mL)	237±11	206±6
AUC0-t (ng·h/mL)	579±49	2079±130
AUC0-∞ (ng·h/mL)	588±36	2090±146
VZ (L/kg)	21.1±2.6
CL ((mL/min)/kg)	57.4±1.3
F (%)		32.5

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