Kevetrin hydrochloride 是一种有效的p53激活剂，可诱导 TP53 野生型和突变型急性髓系白血病细胞凋亡。Kevetrin 对原始胚细胞具有优先的细胞毒性。
| 生物活性 | Kevetrin hydrochloride is a potent activator ofp53, inducesapoptosisin TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells[1][2]. |
体外研究
(In Vitro) | Kevetrin hydrochloride (85, 170, 340 μM; 6 h) significantly inhibits KASUMI-1 cells growth in a dose-dependent manner, without affecting MOLM-13 cells[1].
Kevetrin hydrochloride (340 μM; 6 h) induces metallothionein (MT) expression in acute myeloid leukemia (AML) cells, and also down-regulates genes in relation to p53 activity, the regulator of WNT/β-catenin signaling forkhead box K2 and the transcription factor signal transducer and activator of transcription 5A (STAT5A)[1].
Kevetrin hydrochloride (340 μM; 24 h) induces apoptosis on KASUMI-1 cell line, without leading cell cycle alteration[1].
Kevetrin hydrochloride (100, 200, 400 μM; 48 h) increases the mRNA and protein level of p53 and induces p21 protein production in A2780 cells[1].
Cell Viability Assay[1] | Cell Line: | MOLM-13 and KASUMI-1 cells | | Concentration: | 85, 170 and 340 μM | | Incubation Time: | 6 h, 6 h + 66 h wash-out (wo,×1), 6 h + 66 h wo (×2), 6 h + 66 h wo (×3) | | Result: | Only inhibited the cell viability of KASUMI-1 cells and decreased cells viability in a dose- and time-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | MOLM-13, KASUMI-1, TP53-wt OCI-AML3, and TP53-mutant NOMO-1 cells | | Concentration: | 85, 170 and 340 μM | | Incubation Time: | 24, 48, and 72 hours | | Result: | Induced KASUMI-1 apoptosis at 340 μM on 24 hours and inhibited MOLM-13 at 340 μM on 48 h. |
Cell Cycle Analysis[1] | Cell Line: | MOLM-13, KASUMI-1, TP53-wt OCI-AML3, and TP53-mutant NOMO-1 cells | | Concentration: | 340 μM | | Incubation Time: | 24, and 48 hours | | Result: | Arrested cell cycle of OCI-AML3 and NOMO-1 cells at G0/G1 phase, without altering cell cycle of MOLM-13 and KASUMI-1 cells. |
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体内研究
(In Vivo) | Kevetrin hydrochloride (150-200 mg/kg; i.p.; 20 d) induces ~40% cell death in OV-90 or OVCAR-3 xenograft tumors, also inhibits tumor growth and extents survival time of mice with tumor xenograft mode[2].
| Animal Model: | A2780 xenograft tumor model in nude mice[2] | | Dosage: | 200 mg/kg | | Administration: | Intraperitoneal injection; 3 times per week, for 20 days | | Result: | Inhibited tumor growth and suppressed the tumor volume. |
| Animal Model: | SKOV-3 xenograft ascites model in mice[2] | | Dosage: | 150 mg/kg | | Administration: | Intraperitoneal injection | | Result: | Prolonged the survival time of mice, and maintained 100% survival rate more over 35 days. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(556.58 mM;Need ultrasonic) DMSO : ≥ 40 mg/mL(222.63 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 5.5658 mL | 27.8288 mL | 55.6576 mL | | 5 mM | 1.1132 mL | 5.5658 mL | 11.1315 mL | | 10 mM | 0.5566 mL | 2.7829 mL | 5.5658 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 (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 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： PBS Solubility: 100 mg/mL (556.58 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (13.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (13.91 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (13.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (13.91 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (13.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (13.91 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。 *以上所有助溶剂都可在本网站选购。
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