2378831-21-9
Chemical Structure
DHW-221
- CAS No.: 2378831-21-9
- Formula:C27H22F2N4O5S
- Molecular Weight:552.55
IUPAC Name: 2,4-difluoro-N-(5-(1-(4-(2-hydroxyethoxy)phenyl)-1H-benzo[d]imidazol-6-yl)-2-methoxypyridin-3-yl)benzenesulfonamide
InChIKey: HQDCYADCUBKYSK-UHFFFAOYSA-N
SMILES: O=S(C1=CC=C(F)C=C1F)(NC2=CC(C3=CC=C4C(N(C5=CC=C(OCCO)C=C5)C=N4)=C3)=CN=C2OC)=O
Biological Activity: DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research[1][2][3].
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DHW-221 | DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research. | |||||||||||||||||||||
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References
- [1]. Ding HW, et al. Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors. Bioorg Med Chem. 2019 Jul 1;27(13):2729-2740. [Content Brief]
- [2]. Liu M, et al. DHW-221, a Dual PI3K/mTOR Inhibitor, Overcomes Multidrug Resistance by Targeting P-Glycoprotein (P-gp/ABCB1) and Akt-Mediated FOXO3a Nuclear Translocation in Non-small Cell Lung Cancer. Front Oncol. 2022 May 13;12:873649. [Content Brief]
- [3]. Qin X, et al. Dual blocking of PI3K and mTOR signaling by DHW-221, a novel benzimidazole derivative, exerts antitumor activity in human non-small cell lung cancer. Clin Transl Med. 2021 Sep;11(9):e514. [Content Brief]
