Vps34-PIK-III|cas:1383716-40-2|西域试剂

Vps34-PIK-III,99.02%

产品编号：Bellancom-12794| CAS NO：1383716-40-2| 分子式：C₁₇H₁₇N₇| 分子量：319.36

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12794	￥700.00	杭州北京（现货）
Bellancom-12794	￥1300.00	杭州北京（现货）
Bellancom-12794	￥2100.00	杭州北京（现货）
Bellancom-12794	￥4700.00	杭州北京（现货）
Bellancom-12794	￥8400.00	杭州北京（现货）

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Vps34-PIK-III

产品介绍

Vps34-PIK-III 是一种具有口服活性和选择性的 VPS34 抑制剂 (IC₅₀=18 nM)。Vps34-PIK-III 能有效抑制自噬，可作为分子工具使用。Vps34-PIK-III 也是一种 PI3K 抑制剂，能抑制肝脏癌症干细胞 (CSCs) 基因的表达。

生物活性

Vps34-PIK-III is an orally active and selective VPS34 inhibitor (IC₅₀=18 nM). Vps34-PIK-III effectively inhibits autophagy and can be used as a molecular tool. vps34-PIK-III is also a PI3K inhibitor that inhibits the expression of genes in liver cancer stem cells (CSCs).

体外研究

Vps34-PIK-III (1, 5, 10 µM; 24 h) inhibits autophagy and LC3 lipidation in DLD1 cells.
Vps34-PIK-III (1, 5, 10 µM; 24 h) leads to an increase in the lipidated and nonlipidated forms of LC3 in DLD1 cells.
Vps34-PIK-III (5 µM; 24 h) significantly decreases the expression of stemness genes in HCC cells.
Vps34-PIK-III (5 µM; 24 h) suppresses liver CSCs via AMPK activation in Huh7 and MHCC97H cells.

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

Cell Viability Assay

Cell Line:	DLD1 cells
Concentration:	1, 5, 10 µM
Incubation Time:	24 h
Result:	Prevented the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1.

RT-PCR

Cell Line:	HCC cells
Concentration:	5 µM
Incubation Time:	24 h
Result:	Inhibited stemness genes expression.

Western Blot Analysis

Cell Line:	Huh7 and MHCC97H cells
Concentration:	5 µM
Incubation Time:	24 h
Result:	Inhibited liver CSCs by activating AMPK.

体内研究
(In Vivo)

Vps34-PIK-III (10 mg/kg; p.o.; single) rapidly absorbed and shows moderate mean systemic clearance (30 mL/min/kg, approximately 33% of hepatic blood flow), with good oral bioavailability (F% = 47).

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

Animal Model:

C57BL/6 mice.

Dosage:

10 mg/kg; 2 mg/kg

Administration:

Oral administration; intravenous injection; single

Result:

1.19 Pharmacokinetic Parameters of Vps34-PIK-III in C57BL/6 mice.

	IV (2 mg/kg)	PO (10 mg/kg)
T_max (h)		0.7
C_max (nM)		2994
AUC_inf (nM•h)	2855	6725
t_1/2 (h)	1.2
CL (mL/min/kg)	30
Vdss (L/kg)	1.5
F (%)		47%

体内研究

Vps34-PIK-III (10 mg/kg; p.o.; single) rapidly absorbed and shows moderate mean systemic clearance (30 mL/min/kg, approximately 33% of hepatic blood flow), with good oral bioavailability (F% = 47).

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

Animal Model:

C57BL/6 mice.

Dosage:

10 mg/kg; 2 mg/kg

Administration:

Oral administration; intravenous injection; single

Result:

1.19 Pharmacokinetic Parameters of Vps34-PIK-III in C57BL/6 mice.

	IV (2 mg/kg)	PO (10 mg/kg)
T_max (h)		0.7
C_max (nM)		2994
AUC_inf (nM•h)	2855	6725
t_1/2 (h)	1.2
CL (mL/min/kg)	30
Vdss (L/kg)	1.5
F (%)		47%

体内研究

Vps34-PIK-III (10 mg/kg; p.o.; single) rapidly absorbed and shows moderate mean systemic clearance (30 mL/min/kg, approximately 33% of hepatic blood flow), with good oral bioavailability (F% = 47).

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

Animal Model:

C57BL/6 mice.

Dosage:

10 mg/kg; 2 mg/kg

Administration:

Oral administration; intravenous injection; single

Result:

1.19 Pharmacokinetic Parameters of Vps34-PIK-III in C57BL/6 mice.

	IV (2 mg/kg)	PO (10 mg/kg)
T_max (h)		0.7
C_max (nM)		2994
AUC_inf (nM•h)	2855	6725
t_1/2 (h)	1.2
CL (mL/min/kg)	30
Vdss (L/kg)	1.5
F (%)		47%

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 31 mg/mL (97.07 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1313 mL	15.6563 mL	31.3126 mL
5 mM	0.6263 mL	3.1313 mL	6.2625 mL
10 mM	0.3131 mL	1.5656 mL	3.1313 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 (7.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.83 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 (7.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.83 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 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 (7.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.83 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。