XST-14|cas:2607143-50-8|西域试剂

XST-14,99.69%

产品编号：Bellancom-137506| CAS NO：2607143-50-8| 分子式：C₁₆H₂₁NO₄| 分子量：291.34

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货号	价格	库存与货期
Bellancom-137506	￥2500.00	杭州北京（现货）
Bellancom-137506	￥4500.00	杭州北京（现货）
Bellancom-137506	￥8500.00	杭州北京（现货）
Bellancom-137506	￥13500.00	杭州北京（现货）
Bellancom-137506	￥19500.00	杭州北京（现货）

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XST-14

产品介绍

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。

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.

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

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
(In Vivo)

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.

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

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.

体内研究

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

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.

体内研究

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

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.

性状

Solid

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。
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
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。