XST-14 - CAS:2607143-50-8

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XST-14

目录号 : KM5729 CAS No. : 2607143-50-8 纯度 : 98%

Data Sheet 产品使用指南

XST-14 是一种有效的，竞争性强且高度选择性的 ULK1 抑制剂，IC₅₀ 为 26.6 nM。XST-14 通过减少 ULK1 下游底物的磷酸化来诱导自噬抑制。XST-14 诱导肝细胞癌 (HCC) 细胞凋亡，并具有抗肿瘤作用。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC₅₀ of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.

体外研究

XST-14 inhibits ULK1 (IC₅₀=13.6 nM), MAP2K1/MEK1 (IC₅₀=721.8 nM), MAPK14/p38 alpha (IC₅₀=283.9 nM), TGFBR2 (IC₅₀=809.3 nM), ACVR1/ALK2 (IC₅₀=183.8 nM), ULK2 (IC₅₀=70.9 nM) and CAMK2A (IC₅₀=66.3 nM) by the 10-point titration results from SelectScreen Kinase Profiling Services.
XST-14 (20-80 μM; for 24 h) leads a decrease in cell proliferation activity.
XST-14 (5 μM; for 24 h) induces apoptosis in HepG2 and human primary HCC cells.
XST-14 (5 μM; for 12 h) strongly inhibits the conversion of LC3-I to LC3-II in CHO cells stably expressing GFP-LC3.
XST-14 (5 μM; for 12 h) inhibits the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1.

Cell Proliferation Assay

Cell Line:	HepG2 cells
Concentration:	20, 40, 60, 80 μM
Incubation Time:	24 hours
Result:	Led a decrease in cell proliferation activity.

Apoptosis Analysis

Cell Line:	HepG2 and human primary cells
Concentration:	5 μM
Incubation Time:	24 hours
Result:	Induced apoptosis in HepG2 and human primary HCC cells.

Cell Autophagy Assay

Cell Line:	CHO, HepG2 cells stably expressing GFP-LC3
Concentration:	5 μM
Incubation Time:	12 hours
Result:	Strongly inhibited the conversion of LC3-I to LC3-II in CHO cells. Dramatically decreased the number of GFP-LC3 puncta in HepG2 cells. Decreased autophagosome formation and blocked autophagosome/lysosome fusion in HepG2 cells.

Western Blot Analysis

Cell Line:	HepG2 cells
Concentration:	5 μM
Incubation Time:	12 hours
Result:	Inhibited the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1.

体内研究

XST-14 (15, 30 mg/kg/day; IP; for 4 consecutive weeks) displays anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice.
XST-14 (2 mg/kg for IV; 10 mg/kg for IP) has a T_1/2 of 2.31 hours for IV and a T_1/2 of 2.69 hours for IP.

Animal Model:	Nude mice bearing HepG2 tumor xenografts
Dosage:	15, 30 mg/kg
Administration:	IP; daily; for 4 consecutive weeks
Result:	Displayed anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice.

Animal Model:	Sprague-Dawley rat
Dosage:	2 mg/kg for IV; 10 mg/kg for IP (Pharmacokinetic Analysis)
Administration:	IV or IP
Result:	Had a T_1/2 of 2.31 hours, a CL of 26.28 mL/min•kg, and and an AUC of 1269 hr•ng/mL for IV. Had a T_1/2 of 2.69 hours, a C_max of 2033 ng/mL, and an AUC of 5979 hr•ng/mL for IP.

分子式

C₁₆H₂₁NO₄

分子量

291.34

CAS号

2607143-50-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 250 mg/mL (858.10 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4324 mL	17.1621 mL	34.3242 mL
5 mM	0.6865 mL	3.4324 mL	6.8648 mL
10 mM	0.3432 mL	1.7162 mL	3.4324 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.14 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.14 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。