产品说明书
QCA570
 |
同义名 : | - |
| CAS号 : | 2207569-08-0 | |
| 货号 : | A563444 | |
| 分子式 : | C39H33N7O4S | |
| 纯度 : | 99% | |
| 分子量 : | 695.789 | |
| MDL号 : | N/A | |
| 存储条件： |
粉末 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 40 mg/mL(57.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | QCA570 is a potent PROTAC targeting on BET, consist of an optimized BET ligand QCA276 linked to a CRBN E3 ligand. Treatment with QCA570 led to a dose-dependent depletion of BRD2, 3 and 4 at concentration ranging in 0.01-10nM in MV4;11 and RS4;11 cell lines post 24h, accompanied with downregulation of c-MYC and induction of apoptosis shown by cleaved PARP and Caspase-3. QCA570 exhibited potent anti-proliferation against acute leukemia cell lines with IC50 values of 8.3, 62 and 32pM,for MV4;11, MOLM13, and RS4;11 cell line, respectively, post 96-hour treatment. A good pharmacokinetic and pharmacodynamics properties of QCA570 was shown as a single intravenous dose of 1 or 5mg/kg QCA570 post 24h achieved downregulation of BRD2, 3, 4, c-MYC and increased cleaved PARP in tumors of SCID mice bearing RS4;11. Suppression of tumor growth could be observed in both RS4;11 and MV4;11 xenograft models in mice dosed of QCA570 at 1 or 5 mg/kg, i.v., three times a week for 2 weeks[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.44mL 0.29mL 0.14mL |
7.19mL 1.44mL 0.72mL |
14.37mL 2.87mL 1.44mL |
| 参考文献 |
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