DTP3 TFA 是一种有效且选择性的GADD45β/MKK7抑制剂。DTP3 TFA 靶向 NF-κB 途径下游,具有抗癌活性。
生物活性 | DTP3 TFA is a potent and selectiveGADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7)inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of theNF-κBpathway[1]. |
IC50& Target | |
体外研究 (In Vitro) | DTP3 (10 μM; 1-21 days) causes the potent and tumor-selective induction of JNK activation and apoptosis, as shown by the appearance of phosphorylated JNK, as early as 24 hours[2].
Western Blot Analysis[2] Cell Line: | Multiple myeloma (MM) cell lines | Concentration: | 10 μM | Incubation Time: | 1, 3, 5, 14, 21 days | Result: | Caused the appearance of phosphorylated JNK, as early as 24 hours. |
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体内研究 (In Vivo) | DTP3 TFA (s.c.; 14.5 mg/kg/day; 28 days) has shown a dramatic shrinkage of the tumors, and virtually eradicates established subcutaneous myeloma xenografts in mice[2]. DTP3 TFA (intravenous injection; 10 mg/kg/day) has t1/2of 1.26 hours, CL of 27.13 ML/min/kg, and Vdof 2.80 L/kg[2].
Animal Model: | 6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River)[2] | Dosage: | 14.5 mg/kg | Administration: | S.c.; daily; 28 days | Result: | Had shown a dramatic shrinkage of the tumors. |
Animal Model: | CD1 male mice of 25-30 g[2] | Dosage: | 10 mg/kg (Pharmacokinetic Study) | Administration: | Intravenous injection | Result: | Had t1/2of 1.26 hours, CL of 27.13 ML/min/kg, and Vdof 2.80 L/kg. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture and light Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: H2O : 100 mg/mL(156.34 mM;Need ultrasonic) DMSO : 50 mg/mL(78.17 mM;Need ultrasonic) 配制储备液 1 mM | 1.5634 mL | 7.8171 mL | 15.6343 mL | 5 mM | 0.3127 mL | 1.5634 mL | 3.1269 mL | 10 mM | 0.1563 mL | 0.7817 mL | 1.5634 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 and light)。-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 (156.34 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 (3.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.91 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 (3.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.91 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 (3.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.91 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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