Ceralasertib (AZD6738)

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0 Metric Ton	Negotiable

0 Metric Ton

Negotiable

Min.Order :0 Metric Ton
Purity: >97%

Keywords

Ceralasertib AZD6738 1352226-88-0

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Biological Activity

Description

Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.

Targets

ATR [1]
(Cell-free assay)

1 nM

In vitro

In four Kras mutant cell lines: H23, H460, A549, and H358, AZD6738 inhibits ATR kinase activity and impairs cell viability. In ATM-deficient H23 cells, AZD6738 strongly synergizes with cisplatin to induce rapid cell death. [1] In p53 or ATM defective cells, AZD6738 treatment results in replication fork stalls and accumulation of unrepaired DNA damage, resulting in cell death by mitotic catastrophe. [2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
LICR-LON-HN4 and LICR-LON-HN5 cells	Function assay	0.03, 0.1, 0.3, 1, 3, 10 μM		AZD6738 inhibition of ATR through loss of downstream phosphorylation of CHK1 on Ser345.	30057890
K8484 cells	Function assay	2 μM	7 hours	In K8484 cells, AZD6738 at 2 µM completely prevented gemcitabine-induced Chk1 phosphorylation on Serine 345, the downstream ATR target.	29891488
SNU-601 cells	Cell growth inhibition assay	0-1 μmol/L	5 days	The S and sub-G1 populations of SNU-601 cells were dramatically and dose-dependently increased by AZD6738.	28138034

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Assay

Methods	Test Index	PMID
Western blot	pCHK1 / pCDC25c / pRPA32 / γH2AX / pHH3 / cleaved caspase-3 / RAD51; ATM pSer1981 / ATM / ATR / Chk1 pSer345 / Chk1 / Chk2 pThr68 / Chk2;	29605721 26563132
Immunofluorescence	γH2AX / RAD51; 53BP1;	29605721 26563132
Growth inhibition assay	Cell viability; IC50;	26563132 28062704

In vivo

In nude mice bearing H460 and H23 tumors, AZD6738 (50 mg/kg, p.o.) results in tumor growth inhibition (TGI), and the the combination with cisplatin causes rapid regression of ATM-deficient H23 tumors. [1] In nude mice bearing LoVo xenografts, a combination of AZD6738 (50 mg/kg) + IR (2 Gy) avoids toxicity while still maintaining efficacy. [3]

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