PDK4-IN-1 hydrochloride|cas:2310262-11-2|西域试剂

PDK4-IN-1 hydrochloride,99.51%

产品编号：Bellancom-135954A| CAS NO：2310262-11-2| 分子式：C₂₂H₂₀ClN₃O₂| 分子量：393.87

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货号	价格	库存与货期
Bellancom-135954A	￥3800.00	杭州北京（现货）
Bellancom-135954A	￥5800.00	杭州北京（现货）
Bellancom-135954A	￥16500.00	杭州北京（现货）
Bellancom-135954A	￥23500.00	杭州北京（现货）

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PDK4-IN-1 hydrochloride

产品介绍

PDK4-IN-1 hydrochloride 是一种蒽醌衍生物，也是一种有效的，口服活性的丙酮酸脱氢酶激酶 4 (PDK4) 抑制剂，IC₅₀ 值为 84 nM。PDK4-IN-1 hydrochloride 有效抑制细胞转化和细胞增殖并诱导细胞凋亡 (apoptosis)。PDK4-IN-1 hydrochloride 具有抗糖尿病，抗癌和抗过敏作用。

生物活性

PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC₅₀ value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.

体外研究

PDK4-IN-1 (Compound 8c; 50 μM; 0-72 hours; HCT116 and RKO cells) treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1.
PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis.
PDK4-IN-1 (Compound 8c; 10 μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser²³², Ser²⁹³, and Ser³⁰⁰ of PDHE1α.
10 μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells.
PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1.

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

Cell Viability Assay

Cell Line:	HCT116 and RKO cells
Concentration:	50 μM
Incubation Time:	0 hour, 24 hours, 48 hours, 72hours
Result:	Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO.

Apoptosis Analysis

Cell Line:	HCT116 and RKO cells
Concentration:	10 μM, 25 μM, 50 μM
Incubation Time:	24 hours
Result:	Dose-dependently increased apoptosis.

Western Blot Analysis

Cell Line:	HEK293T human embryonic kidney cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Inhibited phosphorylation of Ser²³², Ser²⁹³, and Ser³⁰⁰ of PDHE1α.

体内研究
(In Vivo)

PDK4-IN-1 (Compound 8c; 100 mg/kg; oral administration; daily; for 1 week; C57BL/6J mice) treatment significantly improves glucose tolerance.
Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10 μM, and 20 μM PDK4-IN-1-treated BMMCs.
The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7 h), and moderate clearance (CL of 0.69) in rats.

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

Animal Model:	C57BL/6J mice (8-week old) fed with high-fat diet
Dosage:	100 mg/kg
Administration:	Oral administration; daily; for 1 week
Result:	Significantly improved glucose tolerance.

体内研究

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

Animal Model:	C57BL/6J mice (8-week old) fed with high-fat diet
Dosage:	100 mg/kg
Administration:	Oral administration; daily; for 1 week
Result:	Significantly improved glucose tolerance.

体内研究

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

Animal Model:	C57BL/6J mice (8-week old) fed with high-fat diet
Dosage:	100 mg/kg
Administration:	Oral administration; daily; for 1 week
Result:	Significantly improved glucose tolerance.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (317.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5389 mL	12.6945 mL	25.3891 mL
5 mM	0.5078 mL	2.5389 mL	5.0778 mL
10 mM	0.2539 mL	1.2695 mL	2.5389 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 (sealed storage, away from moisture)。-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： 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (50.78 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.28 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.28 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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