HDACs/mTOR Inhibitor 1

• CAT Number: I019453
• CAS Number: 2271413-06-8
• Molecular Formula: C28H38N8O5
• Molecular Weight: 566.65
• Purity: ≥95%
• Synonyms: (2R)-N-[4-[1-[7-(hydroxyamino)-7-oxoheptyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-2-methylmorpholine-4-carboxamide
• InChI: InChI=1S/C28H38N8O5/c1-20-19-35(14-17-41-20)28(38)30-22-9-7-21(8-10-22)25-31-26(34-12-15-40-16-13-34)23-18-29-36(27(23)32-25)11-5-3-2-4-6-24(37)33-39/h7-10,18,20,39H,2-6,11-17,19H2,1H3,(H,30,38)(H,33,37)/t20-/m1/s1
• InChIKey: YPXRCUVTZDXVHY-HXUWFJFHSA-N
• SMILES: CC1CN(CCO1)C(=O)NC2=CC=C(C=C2)C3=NC4=C(C=NN4CCCCCCC(=O)NO)C(=N3)N5CCOCC5

HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies[1][2].
HDACs/mTOR Inhibitor 1 (Compound 12l) inhibits leukemia cells proliferation with IC50s of 4.05, 9.01, 9.98 μM for MV4-11, OCI-AML2, OCI-AML3 cells[1].
HDACs/mTOR Inhibitor 1 (0-10 μM, 6 h or 24 h) downregulates p-ERK and increases Ac-H3 in MV4-11 cells[1].
HDACs/mTOR Inhibitor 1 (10 to 1000 nM, 48 h) reduces S-phase cells and increases the percentage of cells in G0/G1 phase in MV4-11 cells[1].
HDACs/mTOR Inhibitor 1 (Compound 12l) (10 or 20 mg/kg, i.v.) inhibits tumor growth without significant toxicity in MV4-11 and MM1S xenograft NOD/SCID mouse model[1].

Reference

[1]. Chen Y, et al. Discovery of a Novel Dual Histone Deacetylases (HDACs) and Mammalian Target of Rapamycin (mTOR) Target Inhibitor as a Promising Strategy for Cancer Therapy. J Med Chem. 2019 Jan 10.
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