| Hazard Information | Back Directory | [Uses]
HDAC-IN-71 (Compound 17q) is a potent HDAC inhibitor with IC50 values of 12.6, 14.1, 20, 3, and 72 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC10, respectively. HDAC-IN-71 induces apoptosis and can be used in cancer research[1]. | [in vivo]
HDAC-IN-71 (100, 200 mg/kg; p.o.; daily; 40 days) inhibits tumor growth at concentrations of 100 mg/kg and 200 mg/kg, with TGI values of 50.92% and 68.00% respectively[1].
Pharmacokinetic analysis[1]
| Parameters | I.V. (2 mg/kg) | P.O. (10 mg/kg) | | AUC0-∞ (h ng/mL) | 1633.35 | 3799.46 | | T1/2 (h) | 3.12 | 2.87 | | CL (L/h/kg) | 1.57 | | | V (L/kg) | 4.63 | | | Cmax(ng/mL) | 851.5 | 774.0 | | F | | 46.52% |
| Animal Model: | Balb/c nude mice[1] | | Dosage: | 100, 200 mg/kg | | Administration: | Oral administration; daily; 40 days | | Result: | Significantly inhibited prostate cancer (PCa) tumor growth. |
| [IC 50]
HDAC1: 12.6 nM (IC50); HDAC2: 14.1 nM (IC50); HDAC3: 20 nM (IC50); HDAC6: 3 nM (IC50); HDAC10: 72 nM (IC50) | [References]
[1] Jiang Q, et al. Discovery of novel itaconimide-based derivatives as potent HDAC inhibitors for the efficient treatment of prostate cancer. Eur J Med Chem. 2024 Apr 5;269:116315. DOI:10.1016/j.ejmech.2024.116315 |
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