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产品名称 | Bax ↓ ↑ | Bcl-2 ↓ ↑ | Bcl-B ↓ ↑ | Bcl-w ↓ ↑ | Bcl-xL ↓ ↑ | Bfl-1 ↓ ↑ | Mcl-1 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BTSA1 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
HA14-1 |
+
Bcl-2, IC50: 9 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Venetoclax |
++++
Bcl-2, Ki: <0.01 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Navitoclax | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
Obatoclax Mesylate |
+++
Bcl-2, Ki: 0.22 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
ABT-737 |
+++
Bcl-2, EC50: 30.3 nM |
+
Bcl-B, EC50: 1.82 μM |
+++
Bcl-w, EC50: 197.8 nM |
+++
Bcl-xL, EC50: 78.7 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
Gambogic Acid |
+
Bfl-1, IC50: 1.06 μM Bcl-2, IC50: 1.21 μM |
++
Bcl-B, IC50: 0.66 μM |
++++
Bcl-w, IC50: 0.02 μM |
+
Bcl-xL, IC50: 1.47 μM |
+
Bfl-1, IC50: 1.06 μM |
++
Mcl-1, IC50: 0.79 μM |
Caspase | {[allProObj[0].p_purity_real_show]} | |||||||||||
BH3I-1 |
+
BH3-Bcl-xL interaction, Ki: 2.4 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
A-1331852 |
++++
Bcl-xL, Ki: <0.01 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
A-1210477 |
++++
MCL-1, IC50: 26.2 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Maritoclax | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
TW-37 |
+++
Bcl-2, Ki: 0.29 μM |
+
Bcl-xL, Ki: 1.11 μM |
+++
Mcl-1, Ki: 0.26 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
UMI-77 |
++
Mcl-1, Ki: 490 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
(R)-(-)-Gossypol acetic acid |
++
Bcl-2, Ki: 0.32 μM |
++
Bcl-xL, Ki: 0.48 μM |
+++
Mcl-1, Ki: 0.18 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
Sabutoclax |
++
Bfl-1, IC50: 0.62 μM Bcl-2, IC50: 0.32 μM |
++
Bcl-xL, IC50: 0.31 μM |
++
Bfl-1, IC50: 0.62 μM |
+++
Mcl-1, IC50: 0.20 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||
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。 |
描述 | DT2216, utilizing PROTAC technology, is a potent and selective degrader of BCL-XL, a member of the Bcl-2 family. It effectively degrades BCL-XL protein by engaging the Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 targets various leukemia and cancer cells dependent on BCL-XL while being significantly less harmful to platelets[1]. |
体内研究 | DT2216 (i.p.; 7.5, 15 mg/kg; weekly for 60 days) shows that the 15 mg/kg dosage is more effective in inhibiting the growth of MOLT-4 T-ALL xenografts in mice compared to the 7.5 mg/kg dosage[1]. |
体外研究 | DT2216 (62.5, 125 nM; 72 hours) is lethal to MOLT-4 cells[1]. DT2216 (0.001-10 μM; 72 hour) is highly toxic to MOLT-4 cells, exhibiting an EC50 of 0.052 μM[1]. DT2216 (0.1, 0.3 μM; 24 hours) induces caspase-3-mediated apoptosis in MOLT-4 cells, relying on the involvement of BCL-2 homologous antagonist killer (BAK) and BCL-2-associated X protein (BAX)[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.65mL 0.13mL 0.06mL |
3.24mL 0.65mL 0.32mL |
6.48mL 1.30mL 0.65mL |
CAS号 | 2365172-42-3 |
分子式 | C77H96ClF3N10O10S4 |
分子量 | 1542.355 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 | |
动物实验配方 |