Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Ceralasertib [1352226-88-0]

Imprimer

Référence NB-64-21458-5mg

Conditionnement : 5mg

Marque : Neo Biotech

Demander plus d'informations

Remove All

Ceralasertib

(Synonyms: AZD6738) Copy Product Info

Synonyms: AZD6738

Catalog No. T3338 Copy Product Info

Purity: 99.99%

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

Cas No. 1352226-88-0

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

Select Batch

Purity:99.99%

Color:White to Yellow

Product Information

Bioactivity

Description	Ceralasertib (AZD6738) is an orally active, selective ATR kinase inhibitor with an IC₅₀ of 1 nM.
Targets & IC50	ATR:1 nM, HT29 cells:2.6 μM (GI50), DYRK (pS421):10.8 μM, A549 cells:2 μM, PI3Kδ:6.8 μM, DYRK:10.8 μM
In vitro	METHODS: 276 different tumor cell lines were treated with Ceralasertib for 3 days and cell viability was measured by MTS assay. RESULTS: For most cell lines, the median GI50 for 50% growth inhibition (1.47 µmol/L) was higher than the IC90 for ATR cells, with only 13% of the cell lines having a GI50 below the median, and 30% below 1 µmol/L. Hematological cell lines (median GI50= 0.82 µmol/L) generally showed increased sensitivity compared to solid tumor cells (median GI50= 1.68 µmol/L). [1] METHODS: Colorectal cancer cells HT29 were treated with trifluridine (70 µM) and Ceralasertib (0.5 µM) for 48 h, and the expression levels of target proteins were measured by Western Blot. RESULTS: The trifluridine+Ceralasertib group inhibited Chk1 phosphorylation in HT29 cells at 48 h compared to the trifluridine group. Therefore, it was confirmed that Ceralasertib inhibited Chk1 phosphorylation. In HT29 and HCT116 cells, DNA damage was more severe in the trifluridine+Ceralasertib group than in the trifluridine group, which could be confirmed by the increased level of γH2A expression. [2]
In vivo	METHODS: To assay anti-tumor activity in vivo, Ceralasertib (10-50 mg/kg, 10% DMSO+40% Propylene Glycol+50% deionized water) was orally administered to LoVo, Granta-519, NCI-H23, or 549 xenograft-carrying athymic nude mice bearing LoVo, Granta-519, NCI-H23 or 549 xenografts once daily for 14-28 days. RESULTS: LoVo and Granta-519 showed dose-dependent efficacy, with significant TGI at 50 mg/kg, moderate activity at 25 mg/kg, and no activity at 10 mg/kg. Significant antitumor activity was also observed in NCI-H23 but not in A549 model. [1]
Synonyms	AZD6738
Kinase Assay	General procedure for the EC50 test: DDR1 is induced by 2 Gg/ml doxycycline for 48 hrs prior to DDR1 activation by rat tail collagen I. The DDR1 over-expressed U2OS is pre-treated by media containing each concentration of the compound for 1 hr and treated by changing the media to the EC50 test media containing 10 Gg/ml collagen and each concentration of the compound for 2 hrs. Each cells is washed with cold PBS three times and lysed with the lysis buffer (50 mMTris, pH 7.5, 1% Triton X-100, 0.1% SDS, 150 mM NaCl, 5 mM EDTA, 100 mMNaF, 2 mM Na3VO4, 1 mM PMSF, 10 Gg/ml aprotinin, and 10 Gg/ml leupeptin). The activation of DDR1 is quantified by density using program ImageJ to determine EC50 following Western blot using anti-activated human DDR1b (Y513).
Cell Research	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 was assessed using the CellTiter-Glo Luminescent Cell Viability Assay and Safire 2 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. GI values, defined as the dose X at which Y = 50%, were extrapolated from dose response curves.

Chemical Properties

Molecular Weight	412.51
Formula	C₂₀H₂₄N₆O₂S
Cas No.	1352226-88-0
Smiles	C[C@@H]1COCCN1c1cc(nc(n1)-c1ccnc2[nH]ccc12)C1(CC1)S(C)(=N)=O
Relative Density.	1.52 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Keep away from moisture,Store at low temperature,Store under nitrogen Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 39 mg/mL (94.54 mM), Sonication is recommended.

DMSO: 250 mg/mL (606.05 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 7.6 mg/mL (18.42 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4242 mL	12.1209 mL	24.2418 mL	121.2092 mL
5 mM	0.4848 mL	2.4242 mL	4.8484 mL	24.2418 mL
10 mM	0.2424 mL	1.2121 mL	2.4242 mL	12.1209 mL
20 mM	0.1212 mL	0.6060 mL	1.2121 mL	6.0605 mL
50 mM	0.0485 mL	0.2424 mL	0.4848 mL	2.4242 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0242 mL	0.1212 mL	0.2424 mL	1.2121 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

Inhibitor.label-data{font-weight:bold;min-width:100px;}.label-data,.data{display:inline-block;min-width:100px;}.description table{word-break:break-all;}.description table td{min-width:200px;}