CNX-1351 is a potent and isoform-selective targeted covalentPI3Kαinhibitor withIC₅₀of 6.8 nM.

CNX-1351 is able to potently (EC₅₀<100 nm) and specifically inhibit signaling in pi3kα-dependent cancer cell lines, this leads to a potent antiproliferative effect (gi₅₀<100 nm). cnx-1351 inhibits pi3k signaling in skov3 cells, with potency (ec₅₀of 10-100 nM) similar to that of the pan-PI3K inhibitor. To investigate the functional consequence of inhibiting PI3Kα in cells, two cell lines with differentPIK3CAactivating mutations, SKOV3 ovarian cancer cells (H1047R) and MCF-7 breast cancer cells (E545K), are treated with CNX-1351 and growth is monitored. BothPIK3CA-driven cell lines are growth inhibited by exposure to CNX-1351 for 96 h (GI₅₀of 78 and 55 nM, respectively)^[1].

CNX-1351 inhibits p-Akt^Ser473in mouse spleens and bonds to PI3Kα in vivo. CNX-1351 is delivered into the intraperitoneal cavity of nude mice at 100 mg/kg once a day for 5 consecutive days (n=3 mice per group). Spleens are harvested from the mice at the indicated times after the last dose (1-24 h) and interrogated by immunoblot for P-Akt^Ser473or for PI3Kα occupancy. Inhibition of PI3K signaling is detected as a decrease in P-Akt^Ser473at 1 and 4 h after last dose^[1].

573.71

Solid

C₃₀H₃₅N₇O₃S

1276105-89-5

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL(174.30 mM;Need ultrasonic)

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.36 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.36 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。