QCA570

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Chemical Structure| 2207569-08-0 同义名 : -
CAS号 : 2207569-08-0
货号 : A563444
分子式 : C39H33N7O4S
纯度 : 99%
分子量 : 695.79
MDL号 : N/A
存储条件：

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

In solvent -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
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

[1]Qin C, Hu Y, et al. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704.