PQR620

目录号: GC32891纯度: >98%
PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure.

PQR620
Cas No.: 1927857-56-4
规格价格库存数量操作
1mg¥563.00现货
1
5mg¥1,328.00现货
1
10mg¥1,935.00现货
1
25mg¥3,297.00现货
1
50mg¥4,467.00现货
1
10mM (in 1mL DMSO)¥1,301.00现货
1

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产品描述 Description

PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure.

PQR620 is a novel brain penetrant dual TORC1/2 inhibitor with anti-tumor activity across 56 lymphoma cell lines with a median IC50 value of 250 nM after 72 h of exposure.[1]

PQR620 has in vivo anti-lymphoma activity and in vivo synergism with the BCL2 inhibitor venetoclax. The combination of PQR620 and venetoclax have stronger in vivo anti-tumor activity than the single agents in a xenograft model of GCB-DLBCL.[1]

[1] Tarantelli C, et al. Cancers (Basel). 2019 Jun 4;11(6).

实验参考方法 Experimental Reference Method

Cell experiment:

The drug concentration causing 50% inhibition of cell proliferation (IC50) is obtained in lymphoma cell lines [diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma (MCL); anaplastic large T-cell lymphoma; and others] exposed to increasing doses of PQR620 for 72 h using a Tecan D300e Digital Dispenser on 384 well plates[2].

Animal experiment:

Mice[2]For in vivo experiments, NOD-Scid (NOD.CB17-Prkdcscid/J) mice are subcutaneously inoculated with 10×106 (RIVA) or with 5×106(SU-DHL-6) cells. Treatments with PQR620 (100mg/kg dose per day, Qdx7/w) started with 100-150 mm3 tumors and are carried for 14 (SU-DHL-6) or 21 days (RIVA).

References:

[1]. Florent Beaufils, et al. Abstract 1336: Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor. Cancer Research; 2016 Apr 16-20.
[2]. Chiara Tarantelli, et al. Targeting the PI3K/mTOR Pathway in Lymphoma with PQR309 and PQR620: Single Agent Activity and Synergism with the BCL2 Inhibitor Venetoclax. Blood 2016 128:3017.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
1927857-56-4
SMILES
[H][C@]1(CC[C@]([H])2COC1)N2C3=NC(N4[C@]5([H])CC[C@]([H])4COC5)=NC(C6=CN=C(N)C=C6C(F)F)=N3
分子式
C21H25F2N7O2
分子量
445.47 g/mol
溶解性
DMSO : 6.4 mg/mL (14.37 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol