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KL-11743

Chemical Structure : KL-11743

CAS No.: 1369452-53-8

KL-11743 (KL11743)

Catalog No.: PC-72556Not For Human Use, Lab Use Only.

KL-11743 (KL11743) is a potent, selective, orally bioavailable inhibitor of class I glucose transporters with IC50 of 115/137/90/68 nM for GLUT1/2/3/4, respectively.

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Biological Activity

KL-11743 (KL11743) is a potent, selective, orally bioavailable inhibitor of class I glucose transporters (GLUT) with IC50 of 115/137/90/68 nM for GLUT1/2/3/4, respectively.
KL-11743 demonstrated no inhibitory activity at 10 uM against hexokinase.
KL-11743 inhibited both glucose consumption, lactate secretion, and 2DG transport in HT-1080 fibrosarcoma cells, with IC50 values of 228, 234, and 87 nM, respectively, and fully inhibited glycolytic ATP production in oligomycin-treated cells with an IC50 of 127 nM.
KL-11743 had minimal off-target activity in a panel of 85 high-liability receptors and transporters and 411 human kinases.
KL-11743 dose-dependently inhibits HT-1080 cells growth (IC50=667 nM), suppresses glucose metabolism and induces redox and energetic stress.
KL-11743 inhibits the growth of TCA cycle-deficient cancers in vitro and in vivo.

Physicochemical Properties

M.Wt 522.609
Formula C30H30N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Acetamide, 2-[3-[6-ethoxy-4-[[4-(1H-pyrazol-4-yl)phenyl]amino]-2-quinazolinyl]phenoxy]-N-(1-methylethyl)-

References

1. Kellen Olszewski, et al. Cell Chem Biol. 2021 Oct 22;S2451-9456(21)00441-4.

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