AZD-4573

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZD-4573 (AZD4573) 是一种有效的选择性 CDK9 抑制剂，与其他激酶（包括其他 CDK 家族激酶）相比，具有快速结合动力学和高选择性。

AZD-4573 (AZD4573) is a potent and selective inhibitor of CDK9, with fast-off binding kinetics and high selectivity versus other kinases, including other CDK family kinases; AZD4573 exhibits a short half-life in multiple preclinical species and good solubility for intravenous administration; dose- and time-dependently decreases cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines; demonstrates in vivo efficacyin xenograft models derived from multiple haematological tumours.Liver Cancer Phase 1 Clinical(In Vitro):Short-term treatment with AZD4573 led to a rapid dose- and time-dependent decrease in cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines (e.g. caspase activation EC50 13.7 nM in an acute myeloid leukemia model MV4-11) .(In Vivo):AZD4573 exhibits a short half-life in multiple species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration.

Short-term treatment with AZD4573 led to a rapid dose- and time-dependent decrease in cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines (e.g. caspase activation EC50 13.7 nM in an acute myeloid leukemia model MV4-11) .

AZD4573 exhibits a short half-life in multiple species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration.

AZD4573

Cell Cycle/DNA Damage

CDK

CDK

Cancer

Liver Cancer

2057509-72-3

429.949

C22H28ClN5O2

>98% (HPLC)

DMSO : ≥ 125 mg/mL 290.74 mM

CC(=O)NC1CCCC(C1)C(=O)NC2=NC=C(C(=C2)C3=C4CC(CN4N=C3)(C)C)Cl

(1S,3R)-3-acetamido-N-(5-chloro-4-(5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl)cyclohexane-1-carboxamide

(-20℃)

With Ice Pack

≥ 2 years