产品
编 号：F756227
分子式：C34H35Cl2N7O3
分子量：660.59
分子式：C34H35Cl2N7O3
分子量：660.59
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CAS No: 2831230-38-5
产品详情
生物活性：
SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch.
体内研究：
SHP2/HDAC-IN-1 (compound 8t, 40 mg/kg, p.o.) inhibits tumor growth in MV4-11 and 4T1 tumor-bearing xenograft mice.SHP2/HDAC-IN-1 (20 mg/kg p.o., 1 mg/kg i.v.) exhibits good maximum plasma concentrations in rats.Animal Model:MV4-11 tumor-bearing xenograft mice
Dosage:40 mg/kg
Administration:Oral adminstration (p.o.), every day for 20 consecutive days.
Result:Delayed tumor progression with a tumor growth inhibition rate (TGI %) value of 64.0%, with no obvious signs of toxicity.
Animal Model:4T1 murine breast cancer model
Dosage:40 mg/kg
Administration:Oral adminstration (p.o.), every day for 12 consecutive days.
Result:Significantly decreased tumor burden with a TGI value of 72%.Increased the proportions of CD4+ T cells and CD8+ T cells in the spleen.Enhanced the proportion of mDCs in lymph nodes.
Animal Model:Male Sprague-Dawley (SD) rats (Pharmacokinetic assay)
Dosage:20 mg/kg p.o., 1 mg/kg i.v.
Administration:Oral adminstration (p.o.) or intravenous injection (i.v.)
Result:Pharmacokinetic profile of SHP2/HDAC-IN-1 (compound 8t). dose (mg/kg) T1/2 (h) Cmax (ng/mL)Cl (mL/h/kg)F (%)
20 (p.o.)5.32183521.42
1 (i.v.)6.153517326
体外研究：
SHP2/HDAC-IN-1 (compound 8t, 0-10 μM approximately, 72 h) inhibits the proliferation of BxPC-3, SW1990, AsPC-1and MV4-11 cells.SHP2/HDAC-IN-1 (0.25-1 μM, 24 h) increases the acetylation of α-tubulin and histone H3 in MV4-11 cells.SHP2/HDAC-IN-1 (0.25 μM, 24 h) inhibits cell cycle progression in the G1 phase of MV4-11 cells.SHP2/HDAC-IN-1 (0.25 and 0.5 μM, 24 h) decreases the mitochondrial membrane potential and activats caspase-3.SHP2/HDAC-IN-1 (2 h) shows good stability in in mouse liver microsome.
SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch.
体内研究：
SHP2/HDAC-IN-1 (compound 8t, 40 mg/kg, p.o.) inhibits tumor growth in MV4-11 and 4T1 tumor-bearing xenograft mice.SHP2/HDAC-IN-1 (20 mg/kg p.o., 1 mg/kg i.v.) exhibits good maximum plasma concentrations in rats.Animal Model:MV4-11 tumor-bearing xenograft mice
Dosage:40 mg/kg
Administration:Oral adminstration (p.o.), every day for 20 consecutive days.
Result:Delayed tumor progression with a tumor growth inhibition rate (TGI %) value of 64.0%, with no obvious signs of toxicity.
Animal Model:4T1 murine breast cancer model
Dosage:40 mg/kg
Administration:Oral adminstration (p.o.), every day for 12 consecutive days.
Result:Significantly decreased tumor burden with a TGI value of 72%.Increased the proportions of CD4+ T cells and CD8+ T cells in the spleen.Enhanced the proportion of mDCs in lymph nodes.
Animal Model:Male Sprague-Dawley (SD) rats (Pharmacokinetic assay)
Dosage:20 mg/kg p.o., 1 mg/kg i.v.
Administration:Oral adminstration (p.o.) or intravenous injection (i.v.)
Result:Pharmacokinetic profile of SHP2/HDAC-IN-1 (compound 8t). dose (mg/kg) T1/2 (h) Cmax (ng/mL)Cl (mL/h/kg)F (%)
20 (p.o.)5.32183521.42
1 (i.v.)6.153517326
体外研究：
SHP2/HDAC-IN-1 (compound 8t, 0-10 μM approximately, 72 h) inhibits the proliferation of BxPC-3, SW1990, AsPC-1and MV4-11 cells.SHP2/HDAC-IN-1 (0.25-1 μM, 24 h) increases the acetylation of α-tubulin and histone H3 in MV4-11 cells.SHP2/HDAC-IN-1 (0.25 μM, 24 h) inhibits cell cycle progression in the G1 phase of MV4-11 cells.SHP2/HDAC-IN-1 (0.25 and 0.5 μM, 24 h) decreases the mitochondrial membrane potential and activats caspase-3.SHP2/HDAC-IN-1 (2 h) shows good stability in in mouse liver microsome.
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