Ceralasertib (AZD6738)

Catalog No.S7693

For research use only.

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

Ceralasertib (AZD6738) Chemical Structure

CAS No. 1352226-88-0

Selleck's Ceralasertib (AZD6738) has been cited by 67 publications

Purity & Quality Control

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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 Formulation Activity Description PMID
LICR-LON-HN4 and LICR-LON-HN5 cells NHPQfHNHfW6ldHnvckBie3OjeR?= MViwMlA{NCByLkGsJFAvOyxiMTygN{whOTBizszN MVHBXmQ3PzN6IHnubIljcXSrb36gc4YhSVSUIITodo92\2hibH;zd{Bw\iCmb4fud5Rz\WGvIIDoc5NxcG:{eXzheIlwdiCxZjDDTGsyKG:wIGPldlM1PS5? NGXGeng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC1O|g6OCd-M{CwOVc5QTB:L3G+
K8484 cells MVPGeY5kfGmxbjDhd5NigQ>? Mom5NkDPxE1? M{jHXFchcG:3coO= NF\RWHdKdiCNOES4OEBk\WyuczygRXpFPjd|ODDheEAzKML3TTDjc41xdGW2ZXz5JJBz\X[nboTl[EBo\W2laYThZolv\S2rbnT1Z4VlKEOqa{GgdIhwe3Cqb4L5cIF1cW:wIH;uJHNmemmwZTCzOFUtKHSqZTDkc5dve3S{ZXHtJGFVWiC2YYLn[ZQv MnXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6OUG0PFgoRjJ7OEmxOFg5RC:jPh?=
SNU-601 cells MmK2R4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjc4PhfS=> MWqwMVEh|ryvb3yvUC=> NECybZc2KGSjeYO= NWPxUGtCXGinIGOgZY5lKHO3Yj3HNUBxd3C3bHH0bY9veyCxZjDTUnUuPjBzIHPlcIx{KHencnWg[JJidWG2aXPhcIx6KGGwZDDkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnZDDifUBCYkR4N{O4Mi=> NVrWTZBrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|gxOzRpPkK4NVM5ODN2PD;hQi=>
breast cancer cell lines M2HBNmNmdGxiZ4Lve5RpKGmwaHnibZRqd25iYYPzZZk> NGTrSFMxNjF{NTygNE4zPSxiMD61JIFv\CBzLkCg{txO NUHkVnlsPSCmYYnz NUKzU5QyUUN3MDD2ZYx2\XNicnHu[4VlKG[{b32gNE4{KHSxIE6xJO69dW:uL1y= NFnSNlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{WwNVEyOyd-Mke1NFEyOTN:L3G+
LoVo cells MYHGeY5kfGmxbjDhd5NigQ>? NYKxO3I3OjRiaB?= NF7nUmZT\WS3Y4Tpc44hcW5iY3XscEBkd3WwdEugZUBxem:yb4L0bY9vKG:oIITo[UBk\WyuIIDvdJVt[XSrb36gZZJmKCirbjDh[IRqfGmxbjD0c{Bk\WyuIHP5Z4xmKGG{cnXzeEkhfW6mZYLnc4lv\yCjcH;weI9{cXNid3jlckBmgHCxc3XkJJRwKGS{dXegZZQh[2:wY3XueJJifGmxboOg[5Jm[XSncjD0bIFvKDQkgJpOwG0> M4PKSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{GwN|EzLz5{NkOxNFMyOjxxYU6=
HT29 cells NFzY[YtHfW6ldHnvckBie3OjeR?= NFztUpE3OCCvaX7z NVLZXFhJUUN3MDC9JFAvODd2IN88US=> NHLxPXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0Olc4Oid-M{CzOFY4PzJ:L3G+
LoVo cells M1nVVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFziN284OiCqcoO= NHzlTJlIUTVyIE2gNE41PCEQvF2= NEPvVWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0Olc4Oid-M{CzOFY4PzJ:L3G+
LoVo cells MVLGeY5kfGmxbjDhd5NigQ>? Mk\JNlUhdWdxa3e= M3TVVFghcHK| M4KwUmNxKD1iMD63OEDPxE1? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-
LoVo cells M{i5NGZ2dmO2aX;uJIF{e2G7 MV21NEBu\y:tZx?= NEO1dlk5KGi{cx?= MWHDdEA:KDJwMjFOwG0> MkfFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
HT-29 cells M3HYRWN6fG:2b4jpZ4l1gSCjc4PhfS=> MkTOO|IhcHK| MV;HTVUxKD1iMj62JO69VQ>? NVXpem4zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFY4PzJpPkOwN|Q3Pzd{PD;hQi=>
LoVo cells MkDuSpVv[3Srb36gZZN{[Xl? MYm3OUBu\y:tZx?= MUK4JIhzew>? M3zs[GNxKD1iMj62JO69VQ>? MlzuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
MDA-MB-468 cells NXrlfoNQTnWwY4Tpc44h[XO|YYm= NXvpdmg3UUN3MDC9JFUvPyEQvF2= M3jmTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{S2O|czLz5|MEO0Olc4OjxxYU6=
Assay
Methods Test Index PMID
Western blot ATM pSer1981 / ATM / ATR / Chk1 pSer345 / Chk1 / Chk2 pThr68 / Chk2 ; pCHK1 / pCDC25c / pRPA32 / γH2AX / pHH3 / cleaved caspase-3 / RAD51 26563132 29605721
Immunofluorescence 53BP1 ; γH2AX / RAD51 26563132 29605721
Growth inhibition assay IC50 ; Cell viability 28062704 26563132
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]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: H23, H460, A549, and H358 cells
  • Concentrations: ~30 μM
  • Incubation Time: 48 h
  • Method: Cells are treated in white walled, clear bottom 96-well plates with the indicated doses of AZD6738, cisplatin, gemcitabine, or combination for 48 h. ATP levels are assessed as surrogate measure of viability is assessed using the CellTiter-Glo Luminescent Cell Viability Assay and Safire2 plate reader. Raw data are corrected for background luminescence prior to further analysis. For AZD6738 treatment, log dose response curves are generated in GraphPad Prism 6 by nonlinear regression (log(inhibitor) vs. response with variable slope) of log-transformed (x = log(x)) data normalized to the mean of untreated controls. GI50 values, defined as the dose X at which Y = 50%, were extrapolated from dose response curves.
Animal Research: [1]
  • Animal Models: Female athymic nude mice bearing H23 or H460 xenografts
  • Dosages: 25 or 50 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 82 mg/mL
(198.78 mM)
Water Insoluble
Ethanol '41 mg/mL warmed

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% propylene glycol+ddH2O
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 412.51
Formula

C20H24N6O2S

CAS No. 1352226-88-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1COCCN1C2=NC(=NC(=C2)C3(CC3)S(=N)(=O)C)C4=C5C=CNC5=NC=C4

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04704661 Recruiting Drug: Ceralasertib|Biological: Trastuzumab Deruxtecan Advanced Breast Carcinoma|Advanced Colon Carcinoma|Advanced Colorectal Carcinoma|Advanced Endometrial Carcinoma|Advanced Gastric Carcinoma|Advanced Gastroesophageal Junction Adenocarcinoma|Advanced Malignant Solid Neoplasm|Advanced Salivary Gland Carcinoma|Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Clinical Stage III Gastric Cancer AJCC v8|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IV Gastric Cancer AJCC v8|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IVA Gastric Cancer AJCC v8|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IVB Gastric Cancer AJCC v8|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8|HER2-Positive Breast Carcinoma|Malignant Hepatobiliary Neoplasm|Metastatic Breast Carcinoma|Metastatic Gastroesophageal Junction Adenocarcinoma|Metastatic Malignant Solid Neoplasm|Pathologic Stage III Gastric Cancer AJCC v8|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIA Gastric Cancer AJCC v8|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIB Gastric Cancer AJCC v8|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIC Gastric Cancer AJCC v8|Pathologic Stage IV Gastric Cancer AJCC v8|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|Stage III Colon Cancer AJCC v8|Stage III Colorectal Cancer AJCC v8|Stage III Major Salivary Gland Cancer AJCC v8|Stage III Uterine Corpus Cancer AJCC v8|Stage IIIA Colon Cancer AJCC v8|Stage IIIA Colorectal Cancer AJCC v8|Stage IIIA Uterine Corpus Cancer AJCC v8|Stage IIIB Colon Cancer AJCC v8|Stage IIIB Colorectal Cancer AJCC v8|Stage IIIB Uterine Corpus Cancer AJCC v8|Stage IIIC Colon Cancer AJCC v8|Stage IIIC Colorectal Cancer AJCC v8|Stage IIIC Uterine Corpus Cancer AJCC v8|Stage IIIC1 Uterine Corpus Cancer AJCC v8|Stage IIIC2 Uterine Corpus Cancer AJCC v8|Stage IV Colon Cancer AJCC v8|Stage IV Colorectal Cancer AJCC v8|Stage IV Major Salivary Gland Cancer AJCC v8|Stage IV Uterine Corpus Cancer AJCC v8|Stage IVA Colon Cancer AJCC v8|Stage IVA Colorectal Cancer AJCC v8|Stage IVA Major Salivary Gland Cancer AJCC v8|Stage IVA Uterine Corpus Cancer AJCC v8|Stage IVB Colon Cancer AJCC v8|Stage IVB Colorectal Cancer AJCC v8|Stage IVB Major Salivary Gland Cancer AJCC v8|Stage IVB Uterine Corpus Cancer AJCC v8|Stage IVC Colon Cancer AJCC v8|Stage IVC Colorectal Cancer AJCC v8|Stage IVC Major Salivary Gland Cancer AJCC v8|Unresectable Colorectal Carcinoma|Unresectable Gastroesophageal Junction Adenocarcinoma|Unresectable Malignant Solid Neoplasm National Cancer Institute (NCI) March 5 2021 Phase 1
NCT04361825 Enrolling by invitation Drug: Durvalumab Small Cell Lung Cancer Samsung Medical Center|AstraZeneca June 17 2020 Phase 2
NCT04298008 Recruiting Drug: AZD6738|Drug: Durvalumab Bile Duct Cancer|Chemotherapy Effect Seoul National University Hospital June 25 2020 Phase 2
NCT04298021 Recruiting Drug: AZD6738|Drug: Durvalumab|Drug: Olaparib Bile Duct Cancer|Chemotherapy Effect Seoul National University Hospital June 25 2020 Phase 2
NCT03669601 Recruiting Drug: AZD6738|Drug: Gemcitabine Cancer CCTU- Cancer Theme|AstraZeneca|Cambridge University Hospitals NHS Foundation Trust October 15 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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