KL-11743

CAS: 1369452-53-8 货号: K646337 分子式: C30H30N6O3 分子量: 522.60
有货
级别和纯度: ≥98%
储存条件
-20°C储存
运输条件
超低温运输
★
规格
库存
价格
数量
1mg
K646337-1mg
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¥1,142.90
5mg
K646337-5mg
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¥3,000.90
10mg
K646337-10mg
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¥4,800.90
25mg
K646337-25mg
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¥9,500.90
50mg
K646337-50mg
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¥14,500.90
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为什么选择此级别

提供 ≥98% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters , with IC 50 s 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 .

In Vitro

KL-11743 (compound 8) competes with glucose for binding to GLUT1, with IC 50 s 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 IC 50 of 677 nM. KL-11743 inhibits the growth of KEAP1 -mutant lung cancer cells with more potency compared to KEAP1 -WT lung cancer cells . 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 IC 50 s of 228, 234, and 87 nM, respectively, and fully inhibited glycolytic ATP production in oligomycin-treated cells with an IC 50 of 127 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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.

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. 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.). MCE 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\n100 mg/kgDosage: 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.

Form:Solid

规格

规格或纯度
≥98%
英文名称
KL-11743
生化机理
KL-11743 是一种强效、口服活性和葡萄糖竞争性的 I 类葡萄糖转运体抑制剂,对 GLUT1、GLUT2、GLUT3 和 GLUT4 的 IC 50 s 分别为 115、137、90 和 68 nM。KL-11743 能特异性地阻断葡萄糖代谢。KL
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
522.60

技术文档

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高级数据

化学和物理性质
溶解性
DMSO : 25 mg/mL (47.84 mM; ultrasonic and warming and heat to 60°C)
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常见问题

本产品的纯度是多少?
本产品的化学纯度(含量)为 ≥98%。批次的具体数值以分析证书(COA)为准。
本产品应如何储存?
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输?
本产品采用保温箱配冰袋运输。收货后请立即拆包,并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少?
本产品的 CAS 号为 1369452-53-8,分子式为 C30H30N6O3,分子量为 522.60 g/mol。
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