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2349356-09-6

中文名称 化合物 T30600
英文名称 BSJ-03-204
CAS 2349356-09-6
分子式 C43H48N10O8
分子量 832.9
MOL 文件 2349356-09-6.mol
更新日期 2024/07/05 14:14:20
2349356-09-6 结构式 2349356-09-6 结构式

基本信息

中文别名
化合物 T30600
英文别名
BSJ-03-204
Acetamide, N-[4-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]butyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-

物理化学性质

密度1.397±0.06 g/cm3(Predicted)
储存条件-20°C, protect from light
溶解度溶于二甲基亚砜
酸度系数(pKa)10.68±0.40(Predicted)
形态Solid
颜色Light yellow to green yellow

常见问题列表

生物活性
BSJ-03-204 是一种有效的,选择性的基于 Palbociclib (HY-50767) 的 CDK4/6 双重降解剂 (PROTAC),对 CDK4/D1 和 CDK6/D1 的 IC50 分别为 26.9 nM 和 10.4 nM。BSJ-03-204 不诱导 IKZF1/3 降解,具有抗癌活性。
靶点

CDK4/D1

26.9 nM (IC 50 )

CDK6/D1

10.4 nM (IC 50 )

体外研究

BSJ-03-204 (0.0001-100 μM; for 3 or 4 days) has potent anti-proliferative effects on MCL cell lines.
BSJ-03-204 (1 μM; for 1 day) potently induces a G1 arrest.
BSJ-03-204 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4/6 in WT cells, not IKZF1/3.

Cell Proliferation Assay

Cell Line: MCL cell lines (Jeko-1, Mino, Granta-519, Rec-1, and Maver-1 cells)
Concentration: 0.0001-100 μM
Incubation Time: For 3 or 4 days
Result: Had potent anti-proliferative effects on mantle cell lymphoma (MCL) cell lines.

Cell Cycle Analysis

Cell Line: Granta-519 cells
Concentration: 1 μM
Incubation Time: For 1 day
Result: Potently induced a G1 arrest.

Western Blot Analysis

Cell Line: Wildtype (WT) or Crbn -/- Jurkat cells
Concentration: 0.1, 0.5, 1, 5 μM
Incubation Time: For 4 hours
Result: Only resulted in degradation of CDK4/6 in WT cells, not IKZF1/3.
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