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
2024/07/22 17:33:51
2349356-09-6 结构式
基本信息
中文别名
化合物 T30600 英文别名
BSJ-03-204Acetamide, 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. |