Cenisertib (Synonyms: AS-703569; R-763) |
| رقم الكتالوجGC35651 |
Cenisertib (AS-703569) هو مثبط متعدد الكيناز منافس لـ ATP والذي يمنع نشاط Aurora-kinase-A / B و ABL1 و AKT و STAT5 و FLT3يحفز Cenisertib تأثيرات مثبطة للنمو عن طريق منع نشاط العديد من الأهداف الجزيئية المختلفة في الخلايا البدينة الورمية (MC)يمنع Cenisertib نمو الورم في نماذج طعم أجنبي من أورام البنكرياس والثدي والقولون والمبيض والرئة وسرطان الدم
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 871357-89-0
Sample solution is provided at 25 µL, 10mM.
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Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC)[1]. Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia[2]. Aurora-A Aurora-B ABL1 Akt STAT5
Cenisertib (AS-703569) (1-1000 nM; for 48 hours) induces dose-dependent inhibition of proliferation in primary neoplastic mast cells (MC) [1].Cenisertib (5-100 nM; for 24 hours) induces a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines[1].Cenisertib (1-1000 nM; for 24 hours)induces apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner[1].Cenisertib (5-500 nM; for 24 hours) induces cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells[1]. Cell Proliferation Assay[1] Cell Line: HMC-1.1, HMC-1.2, ROSAKIT WT, ROSAKIT D816V and MCPV-1.1 mast cells
Cenisertib (AS-703569) (orally; 7 or 10 mg/kg/day; for 3 days) significantly suppresses tumor growth. Animal Model: Female CB17 Severe Combined Immunodeficiency (SCID) mice bearing NCI-MDR tumors[2]
[1]. Peter B, et al. Drug-induced inhibition of phosphorylation of STAT5 overrides drug resistance in neoplastic mast cells. Leukemia. 2018 Apr;32(4):1016-1022. [2]. McLaughlin J, et al. Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.
| Cas No. | 871357-89-0 | SDF | |
| المرادفات | AS-703569; R-763 | ||
| Canonical SMILES | [H][C@@]1([C@H]([C@H]2C(N)=O)NC3=NC(NC4=CC=C(C(C)=C4)N5CCN(CC5)C)=NC=C3F)C[C@]2(C=C1)[H] | ||
| Formula | C24H30FN7O | M.Wt | 451.54 |
| الذوبان | DMSO: 250 mg/mL (553.66 mM) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2146 mL | 11.0732 mL | 22.1464 mL |
| 5 mM | 0.4429 mL | 2.2146 mL | 4.4293 mL |
| 10 mM | 0.2215 mL | 1.1073 mL | 2.2146 mL |
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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
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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