KL-11743|cas:1369452-53-8|西域试剂

KL-11743,98.80%

产品编号：Bellancom-145597| CAS NO：1369452-53-8| 分子式：C₃₀H₃₀N₆O₃| 分子量：522.60

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货号	价格	库存与货期
Bellancom-145597	￥3000.00	杭州北京（现货）
Bellancom-145597	￥4800.00	杭州北京（现货）
Bellancom-145597	￥9500.00	杭州北京（现货）
Bellancom-145597	￥14500.00	杭州北京（现货）

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KL-11743

产品介绍

KL-11743 是一种有效的，具有口服活性的葡萄糖竞争性 I 类葡萄糖转运蛋白抑制剂，抑制 GLUT1，GLUT2，GLUT3 和 GLUT4 的 IC₅₀ 值分别为 115 nM，137 nM，90 nM 和 68 nM。KL-11743 特异性阻断葡萄糖代谢。KL-11743 可与电子传递抑制剂协同诱导细胞死亡。

生物活性

KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC₅₀s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death.

体外研究

KL-11743 (compound 8) competes with glucose for binding to GLUT1, with IC₅₀s of 33 nM and 268 nM at 0.37 mM and 10 mM glucose, respectively.
KL-11743 (39-10000 nM; 24-72 h) dose-dependently inhibits the growth of HT-1080 cells, with an IC₅₀ of 677 nM.
KL-11743 inhibits the growth of KEAP1-mutant lung cancer cells with more potency compared to KEAP1-WT lung cancer cells^[4].
KL-11743 (0.001-10 μM) induces a rapid increase in the phosphorylation of AMPK and acetyl-coenzyme A carboxylase in HT-1080 cells .
KL-11743 (2 μM) inhibits glucose uptake in 786-O cells. KL-11743 increases NADP+/NADPH in NCl-H226 cells. KL-11743 induces cell death in SLC7A11-high cancer cell lines (NCl-H226 and UMRC6 cells).
KL-11743 (0.001-10 μM) inhibits both glucose consumption, lactate secretion, and 2DG transport in HT-1080 fibrosarcoma cells, with IC₅₀s of 228, 234, and 87 nM, respectively, and fully inhibited glycolytic ATP production in oligomycin-treated cells with an IC₅₀ of 127 nM.

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

Cell Viability Assay

Cell Line:	HT-1080 cells
Concentration:	39, 78, 156, 312, 625, 1250, 2500, 5000, 10000 nM
Incubation Time:	24, 48, 72 hours
Result:	Inhibited the growth of HT-1080 cells in a dose-dependent manner.

体内研究
(In Vivo)

KL-11743 (100 mg/kg; i.p. every two days for 5 weeks) decreases the growth of SLC7A11-high NCI-H226 xenograft tumors and was well-tolerated in vivo.
KL-11743 (30-100 mg/kg; a single p.o.) significantly elevates blood glucose levels and delays glucose clearance in mice challenged with 5 g/kg glucose.
KL-11743 significantly suppresses the growth of KEAP1 KO tumors^[4].
Plasma levels of KL-11743 (100 mg/kg; i.p.) are maintained at inhibitory levels for most of the 24-hour dosing period.
KL-11743 (p.o) exhibits moderate oral between 30% and 15%, and favorable and dose-linear plasma exposure profile reaching concentrations of approximately 20 μM in mice (10-100 mg/kg) and rats (10-300 mg/kg).
KL-11743 exhibits comparable half-lives ranging between 2.04 and 5.38 h in rats (10 mg/kg for i.v.; 10-300 mg/kg for p.o.), and 1.45-4.75 h in mice (10 mg/kg for i.v. and i.p.; 10-100 mg/kg for p.o.).

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

Animal Model:	4 to 6-week-old athymic nude mice (Foxn1nu/Foxn1nu) were injected with NCI-H226 cells 100 mg/kg
Dosage:	100 mg/kg
Administration:	I.p. every two days for 5 weeks
Result:	Inhibited the growth of tumors. Exhibited extensive necrotic cell death. Decreased PPP intermediate 6-phosphogluconate levels and increased NADP+/NADPH ratio.

体内研究

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

Animal Model:	4 to 6-week-old athymic nude mice (Foxn1nu/Foxn1nu) were injected with NCI-H226 cells 100 mg/kg
Dosage:	100 mg/kg
Administration:	I.p. every two days for 5 weeks
Result:	Inhibited the growth of tumors. Exhibited extensive necrotic cell death. Decreased PPP intermediate 6-phosphogluconate levels and increased NADP+/NADPH ratio.

体内研究

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

Animal Model:	4 to 6-week-old athymic nude mice (Foxn1nu/Foxn1nu) were injected with NCI-H226 cells 100 mg/kg
Dosage:	100 mg/kg
Administration:	I.p. every two days for 5 weeks
Result:	Inhibited the growth of tumors. Exhibited extensive necrotic cell death. Decreased PPP intermediate 6-phosphogluconate levels and increased NADP+/NADPH ratio.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (47.84 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9135 mL	9.5675 mL	19.1351 mL
5 mM	0.3827 mL	1.9135 mL	3.8270 mL
10 mM	0.1914 mL	0.9568 mL	1.9135 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% corn oil
Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.98 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。