PQR620
产品说明书
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同义名 : | - |
| CAS号 : | 1927857-56-4 | |
| 货号 : | A692574 | |
| 分子式 : | C21H25F2N7O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 445.47 | |
| MDL号 : | MFCD30489733 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | PQR620 is recognized as an orally bioavailable, brain-penetrant inhibitor with selectivity for mTORC1/2. It is a potent mTOR inhibitor, showing over 1000-fold selectivity against PI3Kα in binding assays. In A2058 melanoma cells, PQR620 inhibits phosphorylation of protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) with IC50 values of 0.2 μM and 0.1 μM, respectively. It also displays remarkable selectivity across a broad spectrum of kinases, unrelated receptor enzymes, and ion channels. PQR620's efficacy in halting cancer cell proliferation is demonstrated in an NTRC 44 cancer cell line panel[1]. When tested on 44 lymphoma cell lines, PQR620 has a median IC50 of 250 nM, showing greater activity in B cell tumors compared to T cell tumors (median IC50s: 250 nM vs 450 nM). After 72 hours, PQR620's anti-tumor activity is primarily cytostatic, with apoptosis observed in only 6 out of 44 cell lines (13%). Sensitivity to PQR620 and apoptosis induction are consistent between DLBCL and MCL, unaffected by the DLBCL cell of origin, TP53 status, or the presence of MYC or BCL2 translocations[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.24mL 0.45mL 0.22mL |
11.22mL 2.24mL 1.12mL |
22.45mL 4.49mL 2.24mL |
| 参考文献 |
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