KL-11743 - ≥98% , CAS No.1369452-53-8

CAS: 1369452-53-8 Cat. No.: K646337 Fórmula: C₃₀H₃₀N₆O₃ Peso molecular: 522.60

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

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

Specifications

Especificaciones y pureza

≥98%

Mecanismos bioquímicos y fisiológicos

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-

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Pureza

≥98%

Nombres e identificadores

• Peso molecular: 522.60

Propiedades químicas y físicas

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

Preguntas frecuentes

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1369452-53-8, the molecular formula is C30H30N6O3, and the molecular weight is 522.60 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.