产品
编 号：F276990
分子式：C21H31N5O2
分子量：385.5
分子式：C21H31N5O2
分子量：385.5
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2196204-23-4
产品详情
生物活性：
AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC50 values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a Kd value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL).
体内研究：
AZ1495 (compound 28) (oral, daily, 12.5 mg/kg) leds to tumor regression combination with ibrutinib in an ABC-DLBCL mouse model (OCI-LY10 cells).AZ1495 (iv., 2 mg/kg and oral, 5mg/kg) is characterized by high clearance (Cl) inrat (75 mL/min/kg) and moderate predictions based on hepatocyte data (Clint 15μl/min/106 cells, predicted clearance 42 mL/min/kg) with low bioavailability consistent witha high first pass effect.AZ1495 (iv., 1 mg/kg) has low the amount of active renal secretion occurring in the dog.Animal Model:CB.17 SCID mice
Dosage:12.5 mg/kg
Administration:oral, daily, 12.5 mg/kg
Result:Had modest anti-tumor activity as single agents but a combination ofibrutinib led to tumor regression and is well tolerated.
Animal Model:rat
Dosage:2 mg/kg, 5mg/kg
Administration:iv., 2 mg/kg and oral, 5mg/kg
Result:SpeciesDose (mg/kg)Cl (mL/min/kg)Vss(L/kg)PO halflife (h)IV halflife (h)Fabs (%)F (%)
Rat2，5752.12.00.810028
Dog1293.0-3.3--
Animal Model:dog
Dosage:1 mg/kg
Administration:iv., 1 mg/kg
Result:SpeciesDose (mg/kg)Cl (mL/min/kg)Vss(L/kg)PO halflife (h)IV halflife (h)Fabs (%)F (%)
Rat2，5752.12.00.810028
Dog1293.0-3.3--
体外研究：
AZ1495 (compound 28) (10 μM,1 h) has kinase selectivity for IRAK4 with IC50 values of 0.005 μM (enzyme assay) and 0.052 μM (cellular assay), respectively.AZ1495 (10 μM,1 h) has kinase inhibition for IRAK4 with an IC50 value of 0.005 μM and Kd value of 0.0007 μM.AZ1495 (0.001-100 μM, 72 h) inhibits NF-κB activation and growth of ABC-DLBCL cell lines in a dosedependent manner.AZ1495 (0-3.3 μM, 14 h) completely inhibits NF-κB signaling and induces cell death at lower concentration in combination with a BTK inhibitor in OCI-LY10 cells.
AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC50 values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a Kd value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL).
体内研究：
AZ1495 (compound 28) (oral, daily, 12.5 mg/kg) leds to tumor regression combination with ibrutinib in an ABC-DLBCL mouse model (OCI-LY10 cells).AZ1495 (iv., 2 mg/kg and oral, 5mg/kg) is characterized by high clearance (Cl) inrat (75 mL/min/kg) and moderate predictions based on hepatocyte data (Clint 15μl/min/106 cells, predicted clearance 42 mL/min/kg) with low bioavailability consistent witha high first pass effect.AZ1495 (iv., 1 mg/kg) has low the amount of active renal secretion occurring in the dog.Animal Model:CB.17 SCID mice
Dosage:12.5 mg/kg
Administration:oral, daily, 12.5 mg/kg
Result:Had modest anti-tumor activity as single agents but a combination ofibrutinib led to tumor regression and is well tolerated.
Animal Model:rat
Dosage:2 mg/kg, 5mg/kg
Administration:iv., 2 mg/kg and oral, 5mg/kg
Result:SpeciesDose (mg/kg)Cl (mL/min/kg)Vss(L/kg)PO halflife (h)IV halflife (h)Fabs (%)F (%)
Rat2，5752.12.00.810028
Dog1293.0-3.3--
Animal Model:dog
Dosage:1 mg/kg
Administration:iv., 1 mg/kg
Result:SpeciesDose (mg/kg)Cl (mL/min/kg)Vss(L/kg)PO halflife (h)IV halflife (h)Fabs (%)F (%)
Rat2，5752.12.00.810028
Dog1293.0-3.3--
体外研究：
AZ1495 (compound 28) (10 μM,1 h) has kinase selectivity for IRAK4 with IC50 values of 0.005 μM (enzyme assay) and 0.052 μM (cellular assay), respectively.AZ1495 (10 μM,1 h) has kinase inhibition for IRAK4 with an IC50 value of 0.005 μM and Kd value of 0.0007 μM.AZ1495 (0.001-100 μM, 72 h) inhibits NF-κB activation and growth of ABC-DLBCL cell lines in a dosedependent manner.AZ1495 (0-3.3 μM, 14 h) completely inhibits NF-κB signaling and induces cell death at lower concentration in combination with a BTK inhibitor in OCI-LY10 cells.
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