Ceralasertib (AZD6738)

製品コード: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)化学構造

CAS No. 1352226-88-0

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 44700
JPY 34700
JPY 117700
JPY 246000

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(69)

製品安全説明書

ATM/ATR阻害剤の選択性比較

相関ATM/ATR製品

生物活性

製品説明 Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
ターゲット
ATR [1]
(Cell-free assay)
1 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LICR-LON-HN4 and LICR-LON-HN5 cells NHfpN41HfW6ldHnvckBie3OjeR?= NXfGRppPOC5yMzygNE4yNCByLkOsJFEtKDNuIEGwJO69VQ>? MkPYRXpFPjd|ODDpcohq[mm2aX;uJI9nKEGWUjD0bJJwfWeqIHzvd5Mhd2ZiZH;3cpN1emWjbTDwbI9{eGixconsZZRqd25ib3[gR2hMOSCxbjDT[ZI{PDVw M1ziUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEW3PFkxLz5|MEC1O|g6ODxxYU6=
K8484 cells NHvGc3JHfW6ldHnvckBie3OjeR?= NVfqVWdrOiEQvF2= NUD5TYVzPyCqb4Xydy=> NVjBfI14UW5iS{i0PFQh[2WubIOsJGFbTDZ5M{igZZQhOiEEtV2gZ49ueGyndHXsfUBxemW4ZX70[YQh\2WvY3n0ZYJqdmVvaX7keYNm\CCFaHuxJJBpd3OyaH;yfYxifGmxbjDvckBU\XKrbnWgN|Q2NCC2aHWg[I94dnO2cnXhcUBCXFJidHHy[4V1Ng>? M{DsTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OEmxOFg5Lz5{OUi5NVQ5QDxxYU6=
SNU-601 cells NYrmZ4s6S2WubDDndo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF\h[|gxNTFizsztc4wwVA>? M2TndVUh\GG7cx?= M1T3b3Rp\SCVIHHu[EB{fWJvR{GgdI9xfWyjdHnvcpMhd2ZiU17VMVYxOSClZXzsd{B4\XKnIHTyZY1ifGmlYXzsfUBidmRiZH;z[U1l\XCnbnTlcpRtgSCrbnPy[YF{\WRiYomgRXpFPjd|OD6= NH7hXJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGzPFA{PCd-MkixN|gxOzR:L3G+
breast cancer cell lines NHu2fopE\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHzd4F6 NYXmT2ZJOC5zMkWsJFAvOjVuIECuOUBidmRiMT6wJO69VQ>? MXu1JIRigXN? NY\BO40{UUN3MDD2ZYx2\XNicnHu[4VlKG[{b32gNE4{KHSxIE6xJO69dW:uL1y= Moe3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3MEGxNVMoRjJ5NUCxNVE{RC:jPh?=
LoVo cells M1jiSGZ2dmO2aX;uJIF{e2G7 NV3xS4ZKOjRiaB?= NIfqOmpT\WS3Y4Tpc44hcW5iY3XscEBkd3WwdEugZUBxem:yb4L0bY9vKG:oIITo[UBk\WyuIIDvdJVt[XSrb36gZZJmKCirbjDh[IRqfGmxbjD0c{Bk\WyuIHP5Z4xmKGG{cnXzeEkhfW6mZYLnc4lv\yCjcH;weI9{cXNid3jlckBmgHCxc3XkJJRwKGS{dXegZZQh[2:wY3XueJJifGmxboOg[5Jm[XSncjD0bIFvKDQkgJpOwG0> MlXQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|MUCzNVIoRjJ4M{GwN|EzRC:jPh?=
HT29 cells NHvoVJBHfW6ldHnvckBie3OjeR?= NYe0R24{PjBibXnudy=> NFnOVHdKSzVyIE2gNE4xPzRizszN NYrrdWJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFY4PzJpPkOwN|Q3Pzd{PD;hQi=>
LoVo cells M1S2VmN6fG:2b4jpZ4l1gSCjc4PhfS=> NHfrPY44OiCqcoO= M{HQdWdKPTBiPTCwMlQ1KM7:TR?= M3PDVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{S2O|czLz5|MEO0Olc4OjxxYU6=
LoVo cells MmDpSpVv[3Srb36gZZN{[Xl? MVqyOUBu\y:tZx?= NYjKdGY6QCCqcoO= NFLlZphEeCB;IECuO|Qh|ryP NXi4cIV{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFY4PzJpPkOwN|Q3Pzd{PD;hQi=>
LoVo cells MXzGeY5kfGmxbjDhd5NigQ>? NX3sfXpYPTBibXevb4c> MoXCPEBpenN? MVfDdEA:KDJwMjFOwG0> NXzvUWgzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFY4PzJpPkOwN|Q3Pzd{PD;hQi=>
HT-29 cells MoLtR5l1d3SxeHnjbZR6KGG|c3H5 Mk\LO|IhcHK| Mn[xS2k2OCB;IEKuOkDPxE1? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-
LoVo cells NUPPUVlSTnWwY4Tpc44h[XO|YYm= NXHMbXFSPzVibXevb4c> NGXGSZI5KGi{cx?= NXPGSVhFS3BiPTCyMlYh|ryP MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-
MDA-MB-468 cells NXTBZ5VqTnWwY4Tpc44h[XO|YYm= MWHJR|UxKD1iNT63JO69VQ>? NEX5cGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0Olc4Oid-M{CzOFY4PzJ:L3G+
アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験:[1]
  • 細胞株:H23, H460, A549, and H358 cells
  • 濃度: ~30 μM
  • 反応時間:48 h
  • 実験の流れ: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.
動物試験: [1]
  • 動物モデル:Female athymic nude mice bearing H23 or H460 xenografts
  • 投薬量:25 or 50 mg/kg
  • 投与方法:p.o.

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+40% propylene glycol+ddH2O
混合させたのち直ちに使用することを推奨します。

10mg/mL

化学情報

分子量 412.51
化学式

C20H24N6O2S

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

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05450692 Not yet recruiting Drug: Ceralasertib|Drug: Durvalumab|Drug: Docetaxel Advanced or Metastatic Non-Small Cell Lung Cancer AstraZeneca|Parexel September 15 2022 Phase 3
NCT05061134 Not yet recruiting Drug: Ceralasertib|Biological: Durvalumab Melanoma AstraZeneca July 11 2022 Phase 2
NCT05469919 Recruiting Drug: Ceralasertib Advanced Solid Malignancies AstraZeneca June 9 2022 Phase 1
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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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