[CAS NO. 2057509-72-3]  AZD4573

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PRODUCTS SPECIFICATIONS [2057509-72-3]

Catalog
SLK-S8719
Brand
Selleck
CAS
2057509-72-3

DESCRIPTION [2057509-72-3]

Overview

MDLMFCD31657407
Molecular Weight429.94
Molecular FormulaC22H28ClN5O2
SMILESO=C([C@@H]1C[C@H](NC(C)=O)CCC1)NC2=NC=C(Cl)C(C3=C(CC(C)(C)C4)N4N=C3)=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.3259 mL11.6295 mL23.2591 mL
5 mM0.4652 mL2.3259 mL4.6518 mL
10 mM0.2326 mL1.1630 mL2.3259 mL
50 mM0.0465 mL0.2326 mL0.4652 mL

Description

AZD4573 is a potent inhibitor of (IC50 of <0.004 μM) with fast-off binding kinetics (t = 16 min) and high selectivity versus other kinases, including other CDK family kinases.

Targets

CDK9 [1]
<0.004 μM

In vitro

Short-term treatment with AZD4573 leads 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 0.0137 μM in an acute myeloid leukemia model MV4-11).In human cancer cell line panel screens, AZD4573 demonstrates the ability to induce rapid caspase activation (6h) and loss of viability (24h) across a diverse set of hematological cancers (median caspase EC50 = 30 nM, GI50 = 11 nM) but with minimal effect on solid tumors (median EC50 & GI50 >30 μM).