产品
编 号：F753153
分子式：C29H39N5O5
分子量：537.65
分子式：C29H39N5O5
分子量：537.65
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CAS No: 2482992-54-9
产品详情
生物活性：
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research.
体内研究：
HDAC-IN-36 (compound 23 g) (Zebrafish tumor xenograft model; 0-5 μg/mL, 3 days) shows potent anti-tumor and anti-metastatic activity, and improves in vivo anti-tumor efficacy.HDAC-IN-36 (Beagles, 20 mg/kg, Orally, once) shows a significant improvement in pharmacokinetic parameters.Pharmacokinetic Parameters of HDAC-IN-36 in male Beagles.Parameters23g (20 mg/kg)
T1/2 (h)1.24 ± 0.21
Tmax (h)0.79 ± 0.33
Cmax (μg/L)120.36 ± 15.53
AUC0-t (μg/L?h)1275.35 ± 70.17
AUC0-∞ (μg/L?h)1289.40 ± 88.91
Animal Model:Zebrafish (MDA-MB-231-derived xenograft model, Wild-type AB strain)
Dosage:0, 2.5, 5 μg/mL
Administration:3 days
Result:Inhibited tumor formation and migration in a dose-dependent manner, and improved in vivo anti-tumor efficacy.
Animal Model:Beagles (female, 8-10 kg, n = 4)
Dosage:20 mg/kg (dissolved 0.5% sodium carboxyl methyl cellulose (CMC-Na) aqueous solution)
Administration:Orally, once (Pharmacokinetic Analysis)
Result:Showed a significant improvement in pharmacokinetic parameters with T1/2 value of 1.24 h.
体外研究：
HDAC-IN-36 (compound 23 g) (0-10, 24 h) exhibits good antiproliferative activity in MDA-MB-231 cells, promotes the acetylation of α-Tubulin and HSP90.HDAC-IN-36 (0-10, 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, and mainly induces mitochondrial-dependent apoptosis.HDAC-IN-36 (0-10, 24 h) inhibits MDA-MB-231 cells migration in a dose-dependent manner, increases the expression of E-cadherin and decreases the expression of MMP-2 obviously.HDAC-IN-36 (0-10, 24 h) induces noteworthy autophagy, increases the expression of Beclin1, LC3II and decreases the expression of SQSTM1/p62.
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research.
体内研究：
HDAC-IN-36 (compound 23 g) (Zebrafish tumor xenograft model; 0-5 μg/mL, 3 days) shows potent anti-tumor and anti-metastatic activity, and improves in vivo anti-tumor efficacy.HDAC-IN-36 (Beagles, 20 mg/kg, Orally, once) shows a significant improvement in pharmacokinetic parameters.Pharmacokinetic Parameters of HDAC-IN-36 in male Beagles.Parameters23g (20 mg/kg)
T1/2 (h)1.24 ± 0.21
Tmax (h)0.79 ± 0.33
Cmax (μg/L)120.36 ± 15.53
AUC0-t (μg/L?h)1275.35 ± 70.17
AUC0-∞ (μg/L?h)1289.40 ± 88.91
Animal Model:Zebrafish (MDA-MB-231-derived xenograft model, Wild-type AB strain)
Dosage:0, 2.5, 5 μg/mL
Administration:3 days
Result:Inhibited tumor formation and migration in a dose-dependent manner, and improved in vivo anti-tumor efficacy.
Animal Model:Beagles (female, 8-10 kg, n = 4)
Dosage:20 mg/kg (dissolved 0.5% sodium carboxyl methyl cellulose (CMC-Na) aqueous solution)
Administration:Orally, once (Pharmacokinetic Analysis)
Result:Showed a significant improvement in pharmacokinetic parameters with T1/2 value of 1.24 h.
体外研究：
HDAC-IN-36 (compound 23 g) (0-10, 24 h) exhibits good antiproliferative activity in MDA-MB-231 cells, promotes the acetylation of α-Tubulin and HSP90.HDAC-IN-36 (0-10, 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, and mainly induces mitochondrial-dependent apoptosis.HDAC-IN-36 (0-10, 24 h) inhibits MDA-MB-231 cells migration in a dose-dependent manner, increases the expression of E-cadherin and decreases the expression of MMP-2 obviously.HDAC-IN-36 (0-10, 24 h) induces noteworthy autophagy, increases the expression of Beclin1, LC3II and decreases the expression of SQSTM1/p62.
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