Identification | Back Directory | [Name]
HDACs/mTOR Inhibitor 1 | [CAS]
2271413-06-8 | [Synonyms]
HDACs/mTOR Inhibitor 1 1H-Pyrazolo[3,4-d]pyrimidine-1-heptanamide, N-hydroxy-6-[4-[[[(2R)-2-methyl-4-morpholinyl]carbonyl]amino]phenyl]-4-(4-morpholinyl)- | [Molecular Formula]
C28H38N8O5 | [MDL Number]
MFCD31813768 | [MOL File]
2271413-06-8.mol | [Molecular Weight]
566.65 |
Chemical Properties | Back Directory | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 32.5 mg/mL (57.35 mM; Need ultrasonic) | [form ]
Solid | [pka]
9.47±0.20(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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].
Animal Model: | MV4-11 xenograft NOD/SCID mouse model[1] | Dosage: | 10 mg/kg | Administration: | Intravenous injection (i.v.), every two days (Q2D)×6 | Result: | The TGI (tumor growth inhibitory rate) was 53.1%. |
| [IC 50]
HDAC1: 0.19 nM (IC50); HDAC6: 1.8 nM (IC50); mTOR: 1.2 nM (IC50) | [References]
[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. DOI:10.1021/acs.jmedchem.8b01825 |
|
Company Name: |
MedChemExpress
|
Tel: |
021-58955995 |
Website: |
www.medchemexpress.com |
|