产品
编 号：F715435
分子式：C22H19F2N3O4S
分子量：459.47
分子式：C22H19F2N3O4S
分子量：459.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 2411226-02-1
产品详情
生物活性：
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
体内研究：
BET bromodomain inhibitor 1 (compound 38; 6.25, 12.5 mg/kg; PO; daily ; for 28 days) exhibits stronger antitumor activities and completely inhibits the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg. BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T1/2 of 1.3 and 0.9 hours, a CL of 21.5 and 15.3 mL/min?kg, and a Vss of 1464 and 782 mL/kg for rats and mouse, respectively. BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T1/2 of 3.6 hours, a Cmax of 159 ng/mL and an AUC of 884 ng?h/mL for rats. BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T1/2 of 1.3 hours, a Cmax of 399 ng/mL and an AUC of 1710 ng?h/mL for mouse. Animal Model:An MV4-11 mouse xenograft model
Dosage:6.25, 12.5 mg/kg
Administration:PO; daily ; for 28 days
Result:Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.
Animal Model:Male SD rats
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:IV
Result:Had a T1/2 of 1.3 hours, a CL of 21.5 mL/min?kg, and a Vss of 1464 mL/kg.
体外研究：
BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest.BET bromodomain inhibitor 1 (31.25-500 nM; 6 or 24 hours) is highly effective in inducing dose-dependent inhibition on c-Myc expression and upregulation of p21 levels. BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6. BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC50>20 μM). BET bromodomain inhibitor 1 demonstrates an excellent selectivity for the BET bromodomain family over other bromodomains, with an ～1500-fold selectivity for BRD4(1) over EP300 (IC50=3857 nM). BET bromodomain inhibitor 1 strongly inhibited the growth of acute myeloid leukemia cell line MV4-11, acute leukemia cell lines Kasumi-1 and RS-4-11, and multiple myeloma cancer cell line MM1.S cells with IC50 values of 2.4, 4.8, 17.6 and 15.1 nM, respectively.
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
体内研究：
BET bromodomain inhibitor 1 (compound 38; 6.25, 12.5 mg/kg; PO; daily ; for 28 days) exhibits stronger antitumor activities and completely inhibits the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg. BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T1/2 of 1.3 and 0.9 hours, a CL of 21.5 and 15.3 mL/min?kg, and a Vss of 1464 and 782 mL/kg for rats and mouse, respectively. BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T1/2 of 3.6 hours, a Cmax of 159 ng/mL and an AUC of 884 ng?h/mL for rats. BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T1/2 of 1.3 hours, a Cmax of 399 ng/mL and an AUC of 1710 ng?h/mL for mouse. Animal Model:An MV4-11 mouse xenograft model
Dosage:6.25, 12.5 mg/kg
Administration:PO; daily ; for 28 days
Result:Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.
Animal Model:Male SD rats
Dosage:1 mg/kg (Pharmacokinetic Analysis)
Administration:IV
Result:Had a T1/2 of 1.3 hours, a CL of 21.5 mL/min?kg, and a Vss of 1464 mL/kg.
体外研究：
BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest.BET bromodomain inhibitor 1 (31.25-500 nM; 6 or 24 hours) is highly effective in inducing dose-dependent inhibition on c-Myc expression and upregulation of p21 levels. BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6. BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC50>20 μM). BET bromodomain inhibitor 1 demonstrates an excellent selectivity for the BET bromodomain family over other bromodomains, with an ～1500-fold selectivity for BRD4(1) over EP300 (IC50=3857 nM). BET bromodomain inhibitor 1 strongly inhibited the growth of acute myeloid leukemia cell line MV4-11, acute leukemia cell lines Kasumi-1 and RS-4-11, and multiple myeloma cancer cell line MM1.S cells with IC50 values of 2.4, 4.8, 17.6 and 15.1 nM, respectively.
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