AZD2932 |
رقم الكتالوجGC17959
One-Click Copy Product Info
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AZD2932 هو مثبط كيناز قوي ومتعدد الأهداف VEGFR2 و PDGFβ و Flt-3 و c-Kit مع IC50s من 8 و 4 و 7 و 9 نانومتر في فحص الخلية ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 883986-34-3
Sample solution is provided at 25 µL, 10mM.
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AZD2932 is a potent inhibitor for multiple protein tyrosine kinases (IC50 = 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.) [1]
VEGFR are receptors for vascular endothelial growth factor and belong to receptor tyrosine kinases. It mediates in various cellular functions, including endothelial proliferation, migration, survival, tubular morphogenesis and sprouting. PDGFR are platelet-derived growth factor receptors that exhibit intracellular tyrosine kinase activity. It involves in embryonic development, angiogenesis, proliferation and differentiation etc.
AZD2932 has a potent and balanced profile against PDGFR, VEGFR-2, Flt-3 and c-Kit (IC50: 0.009). It also has a good fraction unbound between 3.3% free in human and 7.0% in dog sera and has no activity against hERG. [1]
In female nude mice bearing C6 tumors, AZD2932 treatment at 3–50 mg/kg b.i.d. 10 h apart give 60–80% inhibition of both p-VEGFR-2 and p-PDGFRb in a 1:1 ratio. [1]
Reference:
1. Plé PA, Jung F, Ashton S, Hennequin L et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6.
Animal experiment: | Mice: To confirm that AZD2932 has similar potency against both PDGFβ and VEGFR-2 phosphorylation, the female nude mice bearing C6 tumors are dosed iv with VEGF-A and PDGFBB 5 min prior to cull and 6 h post last dose of AZD2932 and the lungs excised immediately after. Lung lysates are analyzed by western blot for total and phosphorylated VEGFR-2 and PDGFβ[1]. |
References: [1]. Plé PA, et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6. | |
| Cas No. | 883986-34-3 | SDF | |
| Chemical Name | (Z)-2-(4-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-N-(1-isopropyl-1H-pyrazol-4-yl)acetimidic acid | ||
| Canonical SMILES | CC(N1C=C(/N=C(O)/CC2=CC=C(OC3=NC=NC4=CC(OC)=C(OC)C=C43)C=C2)C=N1)C | ||
| Formula | C24H25N5O4 | M.Wt | 447.49 |
| الذوبان | DMF: 0.25 mg/ml,DMSO: 0.25 mg/ml | 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 | 2.2347 mL | 11.1734 mL | 22.3469 mL |
| 5 mM | 446.9 μL | 2.2347 mL | 4.4694 mL |
| 10 mM | 223.5 μL | 1.1173 mL | 2.2347 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 saline, 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)