KP372-1是一种Akt抑制剂，能抑制癌细胞增殖并诱导细胞凋亡和失巢凋亡。KP372-1 也是一种NQO1氧化还原循环剂，通过产生活性氧 (ROS) 来引起 DNA 损伤 (包括 DNA 断裂)。KP372-1 能有效降低体内肿瘤生长，可用于癌症的研究 (如头颈部鳞状细胞癌和胰腺癌)。
| 生物活性 | KP372-1 is anAktinhibitor that inhibits proliferation and inducesapoptosisand anoikis. KP372-1 is also anNQO1redox cycling agent that causes DNA damage (including DNA breakage) by generating ROS. KP372-1 can be used incancerresearch (such as head and neck squamous cell carcinoma (HNSCC) and pancreatic cancer)[1][2][3]. |
体外研究
(In Vitro) | KP372-1 (0.0625, 0.125, 0.25, 0.5, 1.0 μM; 48 h) inhibits growth of JMARc42 and Tu167c2 cells with IC50s of 200 and 100 nM, respectively[1].
KP372-1 (125 nM; 24 h) induces Tu167c2 cells apoptosis and induces anoikis in the JMARc42 cells[1].
KP372-1 (125 nM; 30 min) blocks Akt, thereby decreasing the phosphorylation of the S6 ribosomal protein in both Tu167 and JMAR cells[1].
KP372-1 (0.250, 0.5, 1.0 μM; 30 min) inhibits Akt kinase activity with an IC50of 250 nM in JMAR cells[1].
Cell Proliferation Assay[1] | Cell Line: | JMARc42 and Tu167c2 cells | | Concentration: | 0.0625, 0.125, 0.25, 0.5, 1.0 μM | | Incubation Time: | 48 h | | Result: | Showed antiproliferative activity. |
Apoptosis Analysis[1] | Cell Line: | Tu167c2 and JMARc42 cells | | Concentration: | 125 nM | | Incubation Time: | 24 h | | Result: | Induced approximately 90% of cells apoptosis. |
Western Blot Analysis[1] | Cell Line: | Tu167 and JMAR cells | | Concentration: | 125 nM | | Incubation Time: | 30 min | | Result: | Induced a small but consistent decrease in Akt phosphorylation with a concomitant marked decrease in S6 phosphorylation.
Inhibited the EGF induced phosphorylation of Aktser473 in Tu167 and AktThr308 in JMAR. |
Western Blot Analysis[1] | Cell Line: | JMAR cells | | Concentration: | 0.250, 0.5, 1.0 μM | | Incubation Time: | 30 min | | Result: | Significantly blocked Akt kinase activity in a dose-dependent fashion, with an IC50of 250 nM. |
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体内研究
(In Vivo) | KP372-1(10, 20 mg/kg; i.v.; single daily for 33 days) induces NADH oxidation and impairs tumor growth in vivo without apparent toxicity[2].
| Animal Model: | Nude mice (H1299 xenografts model)[2]. | | Dosage: | 10, 20 mg/kg | | Administration: | Tailvein injection; single daily for 33 days | | Result: | Affected tumor metabolism and suppressed tumor growth. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 17.86 mg/mL(39.83 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2304 mL | 11.1518 mL | 22.3035 mL | | 5 mM | 0.4461 mL | 2.2304 mL | 4.4607 mL | | 10 mM | 0.2230 mL | 1.1152 mL | 2.2304 mL |
*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。 |
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