FD274

FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16) . FD274 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research[1].

Product Specifications

CAS Number

[2641899-38-7]

UNSPSC

12352005

Target

Apoptosis; mTOR; PI3K

Type

Reference compound

Related Pathways

Apoptosis; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/fd274.html

Purity

99.45

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

ClC1=NC=C(C2=CN=C(NN=C3C4=CC=NC=C4)C3=C2)C=C1NS(=O)(C5=CC=C(F)C=C5)=O

Molecular Formula

C22H14ClFN6O2S

Molecular Weight

480.90

References & Citations

[1]Chengbin Yang, et al. Discovery of N- (2-chloro-5- (3- (pyridin-4-yl) -1H-pyrazolo[3,4-b]pyridin-5-yl) pyridin-3-yl) -4-fluorobenzenesulfonamide (FD274) as a highly potent PI3K/mTOR dual inhibitor for the treatment of acute myeloid leukemia. Eur J Med Chem. 2023 Oct 5;258:115543.