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编 号：F755979
分子式：C25H24N4O
分子量：396.48
分子式：C25H24N4O
分子量：396.48
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CAS No: 2783961-86-2
产品详情
生物活性：
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research.
体内研究：
PRMT5-IN-19 (Compound 41, A375 xenograft model, 75 mg/kg/d, p.o., 19 days) has good PK properties and significant antitumor efficacy, without the obvious loss of body weight and visible toxicity.Animal Model:A375 cell-derived nude mouse xenograft model.
Dosage:75 mg/kg/d
Administration:P.o., 19 days
Result:Had no effect on the body weight, displayed antitumor efficacy with a tumor growth inhibition (TGI) rate of 73% by inhibiting the methyltransferase activity of PRMT5.
Animal Model:Rats and mice.
Dosage:10 mg/kg for p.o., 3 mg/kg for i.v
Administration:P.o., i.v. (Pharmacokinetic Analysis)
Result:Pharmacokinetic parameters for PRMT5-IN-19 in SD Rats and Micea,c .speciesPRMT5-IN-19 T1/2 (h)Cmax (ng/mL)CL (mL/min/kg) F (%)
rativ (3 mg/kg)/td>2.58310
po (10 mg/kg)/td>7.518.22 7.25
po (10 mg/kg)/td>2.9527.7 23.7
mouseiv (3 mg/kg)/td>4.71 153
po (10 mg/kg)/td> 128
体外研究：
PRMT5-IN-19 (Compound 41, 5 days) has strong anti-proliferative effects against the A375 cell with an IC50 value of 1.36 μM.PRMT5-IN-19 shows higher selectivity for PRMT5 (IC50 value of 23.9 nM) than other histone methyltransferases (PRMT1 and PRMT4), and PKMTS (EZH2, NSD2, MLL1, and MLL4) .PRMT5-IN-19 binds with the SAM-binding pocket in PRMT5.PRMT5-IN-19 (4-5 days) Inhibits proliferation of multiple cancer cell lines (A-375, CHL-1, SNU-423, SNU-449, MDA-MB-231, MDA-MA-453, MV-4-11, MOLM13) with IC50 value ranging from 1.08 to 3.45 μM.PRMT5-IN-19 inhibits arginine symmetrical dimethylation in A375 cells .PRMT5-IN-19 (0-4 μM, 48 h) suppresses A375 cell proliferation by inducing apoptosis in a concentration-dependent manner.
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research.
体内研究：
PRMT5-IN-19 (Compound 41, A375 xenograft model, 75 mg/kg/d, p.o., 19 days) has good PK properties and significant antitumor efficacy, without the obvious loss of body weight and visible toxicity.Animal Model:A375 cell-derived nude mouse xenograft model.
Dosage:75 mg/kg/d
Administration:P.o., 19 days
Result:Had no effect on the body weight, displayed antitumor efficacy with a tumor growth inhibition (TGI) rate of 73% by inhibiting the methyltransferase activity of PRMT5.
Animal Model:Rats and mice.
Dosage:10 mg/kg for p.o., 3 mg/kg for i.v
Administration:P.o., i.v. (Pharmacokinetic Analysis)
Result:Pharmacokinetic parameters for PRMT5-IN-19 in SD Rats and Micea,c .speciesPRMT5-IN-19 T1/2 (h)Cmax (ng/mL)CL (mL/min/kg) F (%)
rativ (3 mg/kg)/td>2.58310
po (10 mg/kg)/td>7.518.22 7.25
po (10 mg/kg)/td>2.9527.7 23.7
mouseiv (3 mg/kg)/td>4.71 153
po (10 mg/kg)/td> 128
体外研究：
PRMT5-IN-19 (Compound 41, 5 days) has strong anti-proliferative effects against the A375 cell with an IC50 value of 1.36 μM.PRMT5-IN-19 shows higher selectivity for PRMT5 (IC50 value of 23.9 nM) than other histone methyltransferases (PRMT1 and PRMT4), and PKMTS (EZH2, NSD2, MLL1, and MLL4) .PRMT5-IN-19 binds with the SAM-binding pocket in PRMT5.PRMT5-IN-19 (4-5 days) Inhibits proliferation of multiple cancer cell lines (A-375, CHL-1, SNU-423, SNU-449, MDA-MB-231, MDA-MA-453, MV-4-11, MOLM13) with IC50 value ranging from 1.08 to 3.45 μM.PRMT5-IN-19 inhibits arginine symmetrical dimethylation in A375 cells .PRMT5-IN-19 (0-4 μM, 48 h) suppresses A375 cell proliferation by inducing apoptosis in a concentration-dependent manner.
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