BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity.


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| 产品名称 | Cdc ↓ ↑ | CDK1 ↓ ↑ | CDK19 ↓ ↑ | CDK2 ↓ ↑ | CDK3 ↓ ↑ | CDK4 ↓ ↑ | CDK5 ↓ ↑ | CDK6 ↓ ↑ | CDK7 ↓ ↑ | CDK8 ↓ ↑ | CDK9 ↓ ↑ | CLK ↓ ↑ | 其他靶点 | 纯度 | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| XL413 HCl |
++++
Cdc7, IC50: 3.4 nM |
99%+ | |||||||||||||||||
| SU9516 |
+++
CDK1, IC50: 40 nM |
+++
CDK2, IC50: 22 nM |
++
CDK4, IC50: 200 nM |
99%+ | |||||||||||||||
| RO-3306 |
+++
CDK1, Ki: 20 nM |
ERK,SGK | 98% | ||||||||||||||||
| R547 |
++++
CDK1/CyclinB, Ki: 2 nM |
++++
CDK2/CyclinE, Ki: 3 nM |
++++
CDK4/CyclinD1, Ki: 1 nM |
99%+ | |||||||||||||||
| BMS-265246 |
++++
CDK1/CyclinB, IC50: 6 nM |
++++
CDK2/CyclinE, IC50: 9 nM |
+
CDK4/CyclinD, IC50: 230 nM |
99%+ | |||||||||||||||
| NU6027 |
+
CDK1, Ki: 2.5 μM |
+
CDK2, Ki: 1.3 μM |
DNA-PK | 98% | |||||||||||||||
| Purvalanol A |
++++
Cdc2/CyclinB, IC50: 4 nM |
+++
CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM |
+
CDK4/CyclinD1, IC50: 850 nM |
99%+ | |||||||||||||||
| SCH900776 |
++
CDK2, IC50: 0.16 μM |
99%+ | |||||||||||||||||
| AUZ 454 |
++++
CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM |
99%+ | |||||||||||||||||
| A-674563 HCl |
++
CDK2, Ki: 46 nM |
PKA | 99% | ||||||||||||||||
| JNJ-7706621 |
++++
CDK1/CyclinB, IC50: 9 nM |
++++
CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM |
++
CDK3/CyclinE, IC50: 58 nM |
+
CDK4/CyclinD1, IC50: 253 nM |
++
CDK6/CyclinD1, IC50: 175 nM |
99%+ | |||||||||||||
| AT7519 |
++
CDK1/CyclinB, IC50: 210 nM |
++
CDK2/CyclinA, IC50: 47 nM |
+
CDK3/CyclinE, IC50: 360 nM |
++
CDK4/CyclinD1, IC50: 100 nM |
+++
CDK5/p35, IC50: 13 nM |
++
CDK6/CyclinD3, IC50: 170 nM |
++++
CDK9/CyclinT, IC50: <10 nM |
98+% | |||||||||||
| PHA-793887 |
++
CDK1/CyclinB, IC50: 60 nM |
++++
CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM |
++
CDK4/CyclinD1, IC50: 62 nM |
++++
CDK5/p25, IC50: 5 nM |
++++
CDK7/CyclinH, IC50: 10 nM |
++
CDK9/CyclinT1, IC50: 138 nM |
99%+ | ||||||||||||
| Milciclib |
+
CDK1/CyclinB, IC50: 398 nM |
++
CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM |
++
CDK4/CyclinD1, IC50: 160 nM |
+
CDK5/p35, IC50: 265 nM |
++
CDK7/CyclinH, IC50: 150 nM |
99%+ | |||||||||||||
| Kenpaullone |
+
CDK1/CyclinB, IC50: 0.4μM |
+
CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM |
+
CDK5/p35, IC50: 0.85μM |
98% | |||||||||||||||
| SNS-032 |
+++
CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM |
+
CDK5/p35, IC50: 340 nM |
++
CDK7/CyclinH, IC50: 62 nM |
++++
CDK9/CyclinT, IC50: 4 nM |
99%+ | ||||||||||||||
| Dinaciclib |
++++
CDK1, IC50: 3 nM |
++++
CDK2, IC50: 1 nM |
++++
CDK5, IC50: 1 nM |
++++
CDK9, IC50: 4 nM |
99%+ | ||||||||||||||
| PHA-767491 HCl |
++++
Cdc7, IC50: 10 nM |
+
CDK1, IC50: 250 nM |
+
CDK2, IC50: 240 nM |
+
CDK5, IC50: 460 nM |
+++
CDK9, IC50: 34 nM |
MK2 | 99% | ||||||||||||
| (R)-Roscovitine |
+
Cdc2/CyclinB, IC50: 0.65 μM |
+
CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM |
++
CDK5/p35, IC50: 0.16 μM |
99%+ | |||||||||||||||
| Narazaciclib |
++++
CDK4/CyclinD1, IC50: 3.87 nM |
++++
CDK6/CyclinD1, IC50: 9.82 nM |
RET | 99%+ | |||||||||||||||
| Palbociclib |
++++
CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM |
+++
CDK6/CyclinD2, IC50: 15 nM |
99% | ||||||||||||||||
| Abemaciclib |
++++
CDK4, IC50: 2 nM |
++++
CDK6, IC50: 10 nM |
99% | ||||||||||||||||
| Ribociclib |
++++
CDK4, IC50: 10 nM |
+++
CDK6, IC50: 39 nM |
98% | ||||||||||||||||
| Palbociclib isethionate |
++++
CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM |
+++
CDK6/CyclinD2, IC50: 15 nM |
99%+ | ||||||||||||||||
| BS-181 HCl |
+++
CDK7, IC50: 21 nM |
99%+ | |||||||||||||||||
| (E/Z)-THZ1 2HCl |
++++
CDK7, IC50: 3.2 nM |
99%+ | |||||||||||||||||
| LDC4297 |
++++
CDK7, IC50: 0.13 nM |
99%+ | |||||||||||||||||
| Senexin A |
+
CDK19, Kd: 0.31 μM |
+
CDK8, Kd: 0.83 μM |
99% | ||||||||||||||||
| MSC2530818 |
++++
CDK8, IC50: 2.6 nM |
99%+ | |||||||||||||||||
| Wogonin | ✔ | 99%+ | |||||||||||||||||
| Riviciclib HCl |
++
CDK1/CyclinB, IC50: 79 nM |
+
CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM |
++
CDK4/CyclinD1, IC50: 63 nM |
+
CDK6/CyclinD3, IC50: 396 nM |
+
CDK7/CyclinH, IC50: 2.87 μM |
+++
CDK9/CyclinT1, IC50: 20 nM |
98% | ||||||||||||
| LDC000067 |
+
CDK2, IC50: 2.441 μM |
++
CDK9, IC50: 44 nM |
98% | ||||||||||||||||
| Flavopiridol |
+++
CDK1, IC50: 40 nM |
+++
CDK2, IC50: 40 nM |
+++
CDK4, IC50: 40 nM |
+++
CDK6, IC50: 40 nM |
+
CDK7, IC50: 300 nM |
+++
CDK9, IC50: 20 nM |
99%+ | ||||||||||||
| LY2857785 |
+
CDK7, IC50: 0.246 μM |
+++
CDK8, IC50: 0.016 μM |
+++
CDK9, IC50: 0.011 μM |
99%+ | |||||||||||||||
| AZD-5438 |
+++
CDK1, IC50: 16 nM |
++++
CDK2, IC50: 6 nM |
+++
CDK9, IC50: 20 nM |
99%+ | |||||||||||||||
| ML167 |
++
Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM |
99%+ | |||||||||||||||||
| (E/Z)-TG003 |
+++
mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM |
99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.20mL 0.24mL 0.12mL |
6.00mL 1.20mL 0.60mL |
12.01mL 2.40mL 1.20mL |
|
| CAS号 | 2349356-09-6 |
| 分子式 | C43H48N10O8 |
| 分子量 | 832.9 |
| SMILES Code | O=C(NCCCCN1CCN(C2=CN=C(C=C2)NC=3N=CC4=C(N3)N(C(=O)C(C(=O)C)=C4C)C5CCCC5)CC1)COC6=CC=CC=7C(=O)N(C(=O)C67)C8C(=O)NC(=O)CC8 |
| MDL No. | MFCD33023229 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
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