JX06|cas:729-46-4|西域试剂

JX06,99.88%

产品编号：Bellancom-19564| CAS NO：729-46-4| 分子式：C₁₀H₁₆N₂O₂S₄| 分子量：324.51

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货号	价格	库存与货期
Bellancom-19564	￥500.00	杭州北京（现货）
Bellancom-19564	￥800.00	杭州北京（现货）
Bellancom-19564	￥1800.00	杭州北京（现货）
Bellancom-19564	￥3000.00	杭州北京（现货）
Bellancom-19564	￥5000.00	杭州北京（现货）

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JX06

产品介绍

JX06 是一种有效的，选择性的，共价的 PDK 抑制剂。JX06 抑制 PDK1, PDK2 和 PDK3，IC₅₀ 值分别为 49 nM，101 nM 和 313 nM。JX06 以不可逆的方式与半胱氨酸残基共价结合来抑制 PDK1 活性。JX06 具有抗肿瘤活性。

生物活性

JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC₅₀s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.

体外研究

JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM.
JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR.
JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells.
JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner.
JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells.
JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line:	A549, EBC-1, HT-29 and H460 cells
Concentration:	0, 1, 3, 10 μM
Incubation Time:	48 hours
Result:	Induces cell apoptosis in A549 and EBC-1 cells.

Cell Viability Assay

Cell Line:	A549 cells
Concentration:	0, 0.2, 0.4, 0.6 μM
Incubation Time:	72 hours
Result:	Inhibits the viability of A549 cells in a dose dependent manner.

Western Blot Analysis

Cell Line:	A549 cells
Concentration:	0, 0.1, 0.3, 1, 3, 10 μM
Incubation Time:	0, 6, 12, 24 hours
Result:	Decreased PDHA1 phosphorylation at both serine 293 and serine 232 (S293 and S232) in a time- and dose-dependent manner.

体内研究
(In Vivo)

JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	A549 subcutaneous xenograft mice
Dosage:	40, 80 mg/kg
Administration:	I.p. injections for 21 days
Result:	Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control. Well tolerated at the administration dose.

体内研究

JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	A549 subcutaneous xenograft mice
Dosage:	40, 80 mg/kg
Administration:	I.p. injections for 21 days
Result:	Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control. Well tolerated at the administration dose.

体内研究

JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	A549 subcutaneous xenograft mice
Dosage:	40, 80 mg/kg
Administration:	I.p. injections for 21 days
Result:	Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control. Well tolerated at the administration dose.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (154.08 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0816 mL	15.4078 mL	30.8157 mL
5 mM	0.6163 mL	3.0816 mL	6.1631 mL
10 mM	0.3082 mL	1.5408 mL	3.0816 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°C, 6 months; -20°C, 1 month。-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。

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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.70 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% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (7.70 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.70 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.70 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。