AZD6738 (Synonyms: Ceralasertib) |
| Catalog No.GC16941 |
AZD6738 (AZD6738) es un inhibidor biodisponible y activo por vÍa oral de la quinasa ATR con una IC50 de 1 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1352226-88-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
AZD6738 is a selective ATR (Ataxia Telangiectasia and RAD3-related) inhibitor, with an IC50 of approximately 30 uM to resting CLL cells [1] [2].
ATR is a PI3K-related kinase. It is involved in the repair of DNA damage. During cell division, it is recruited and activated at sites of single strand DNA breaks to help initiate DNA repair [1].
γH2AX acts as a biomarker of DNA damage. In an in vitro model capable of reproducing, over 70 hours after the initiation of the treatment with AZD6738, the γH2AX signal was sustained [1]. Stalled replication forks may collapse the formation of DNA double stranded breaks and the activation of the ataxia telangiectasia mutated (ATM) kinase. As a single agent across cancer cell line panels, AZD6738 is active. In cell lines lacking ATM-pathway, the sensitivity of AZD6738 was enhanced [3].
In ATM-deficient but not ATM-proficient in vivo models, treatment with AZD6738 alone significantly inhibited the activity of tumors in equivalent, tolerated doses. Ionizing radiation (IR) is a DNA damaging inducing agent. When AZD6738 and IR were used together, regression or anti-tumor growth inhibitory activity was observed. In tumor tissue, AZD6738 is associated with a persistent γH2AX staining increase. In normal gut tissue or bone marrow, treatment with AZD6738 only transiently increased the γH2AX staining [3].
References:
[1]. Choi MY, Fecteau JF, Brown J, et al. Induction of proliferation sensitizes chronic lymphocytic leukemia cells to apoptosis mediated by the ATR inhibitor AZD6738. Cancer Research, 2014, 74(19 Supplement): 5485-5485.
[2]. Checkley S, MacCallum L, Yates J, et al. Bridging the gap between in vitro and in vivo: Dose and schedule predictions for the ATR inhibitor AZD6738. Scientific reports, 2015, 5.
[3]. Guichard SM, Brown E, Odedra R, et al. The pre-clinical in vitro and in vivo activity of AZD6738: A potent and selective inhibitor of ATR kinase. Cancer Research, 2013, 73(8 Supplement): 3343-3343.
Cell experiment: | Ceralasertib (AZD6738) is dissolved in DMSO at 30 mM and diluted in DMSO to desired working concentrations. The final DMSO concentration in media for all conditions and controls is 0.1% for Ceralasertib (AZD6738) dose response experiments, 0.05% for Ceralasertib (AZD6738) + chemotherapy viability experiments, and 0.025% for all experiments involving 0.3 μM and 1.0 μM doses of Ceralasertib (AZD6738)[1]. |
Animal experiment: | Mice[1]Ceralasertib (AZD6738) is dissolved in DMSO at a concentration of 25 mg/mL or 50 mg/mL and diluted 1:5 in propylene glycol. Ceralasertib (AZD6738) is administered by oral gavage at 25 mg/kg (H23) or 50 mg/kg (H460) for 14 consecutive days. The dosing volume is 10 mL/kg.[1]. |
References: [1]. Vendetti FP, et al. The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of CDDP to resolve ATM-deficient non-small cell lung cancer in vivo. | |
| Cas No. | 1352226-88-0 | SDF | |
| Sinónimos | Ceralasertib | ||
| Chemical Name | (R)-3-methyl-4-(6-(1-((R)-S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl)morpholine | ||
| Canonical SMILES | C[C@H]1N(C2=NC(C3=C4C(NC=C4)=NC=C3)=NC(C5([S@](=O)(C)=N)CC5)=C2)CCOC1 | ||
| Formula | C20H24N6O2S | M.Wt | 412.51 |
| Solubility | ≥ 82 mg/mL in DMSO, ≥ 82.4 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4242 mL | 12.1209 mL | 24.2418 mL |
| 5 mM | 0.4848 mL | 2.4242 mL | 4.8484 mL |
| 10 mM | 0.2424 mL | 1.2121 mL | 2.4242 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *