产品
编 号：F156732
分子式：C15H15FN6O2S2
分子量：394.45
分子式：C15H15FN6O2S2
分子量：394.45
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
2mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1421693-22-2
产品详情
生物活性：
Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion.
体内研究：
Asnuciclib (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities..Animal Model:MV4-11 tumor bearing mice.
Dosage:25 mg/kg.
Administration:Orally once everyday for 33 days.
Result:Caused a remarkable delay in tumor growth compared to vehicle-treated mice, as reflected in a percentage for the mean tumor volume in treated to control mice of 43% at day 31.
Animal Model:Balb/C mice aged 6-8 weeks.
Dosage:2 mg/kg (IV), 10, 20 and 40 mg/kg (PO). (Pharmacokinetic Analysis.)
Administration:IV and PO, single dose.
Result:The Cmax increased from 1.29 to 3.66 μM at a mean time of 1 h and the area under the curve (AUC) of CDKI-73 increased from 3.51 to 12.8 μM.h when the oral dose was escalated from 10 to 40 mg/kg. CDKI-73 was eliminated from plasma with a mean terminal half-life (T1/2) of 2 h. Its oralbioavailability (F) ranged from 54 to 85% across the three doses.
体外研究：
Asnuciclib is highly cytotoxic to primary leukemia cells derived from CLL patients (mean LD50 = 0.08 μM) and shows>500-fold selectivity for primary leukemia cells over normal B-lymphocytes (LD50=40.5 μM).Asnuciclib (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells.Asnuciclib induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II.Asnuciclib is highly effective against all cell lines tested with an IC50 in the range of 0.012-0.517 μM; in particular three MLL-AML cell lines, namely MOLM13, MV4-11 and THP-1, were highly sensitive to CDKI-73 with IC50 values Asnuciclib 相关抗体:Cell Viability Assay.Cell Line:CLL cells.
Concentration:0-1 μM.
Incubation Time:48 h.
Result:Shows preferential cytotoxicity in CLL cells.
Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion.
体内研究：
Asnuciclib (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities..Animal Model:MV4-11 tumor bearing mice.
Dosage:25 mg/kg.
Administration:Orally once everyday for 33 days.
Result:Caused a remarkable delay in tumor growth compared to vehicle-treated mice, as reflected in a percentage for the mean tumor volume in treated to control mice of 43% at day 31.
Animal Model:Balb/C mice aged 6-8 weeks.
Dosage:2 mg/kg (IV), 10, 20 and 40 mg/kg (PO). (Pharmacokinetic Analysis.)
Administration:IV and PO, single dose.
Result:The Cmax increased from 1.29 to 3.66 μM at a mean time of 1 h and the area under the curve (AUC) of CDKI-73 increased from 3.51 to 12.8 μM.h when the oral dose was escalated from 10 to 40 mg/kg. CDKI-73 was eliminated from plasma with a mean terminal half-life (T1/2) of 2 h. Its oralbioavailability (F) ranged from 54 to 85% across the three doses.
体外研究：
Asnuciclib is highly cytotoxic to primary leukemia cells derived from CLL patients (mean LD50 = 0.08 μM) and shows>500-fold selectivity for primary leukemia cells over normal B-lymphocytes (LD50=40.5 μM).Asnuciclib (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells.Asnuciclib induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II.Asnuciclib is highly effective against all cell lines tested with an IC50 in the range of 0.012-0.517 μM; in particular three MLL-AML cell lines, namely MOLM13, MV4-11 and THP-1, were highly sensitive to CDKI-73 with IC50 values Asnuciclib 相关抗体:Cell Viability Assay.Cell Line:CLL cells.
Concentration:0-1 μM.
Incubation Time:48 h.
Result:Shows preferential cytotoxicity in CLL cells.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备