ZM 306416 (Synonyms: CB-676475) |
カタログ番号GC12185
One-Click Copy Product Info
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ZM-306416 (CB 676475) は VEGFR の強力な阻害剤であり、KDR と Flt の IC50 はそれぞれ 0.1 と 2 μM です。 ZM-306416 は、IC50 が 10 nM 未満の EGFR 阻害剤でもあります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 690206-97-4
Sample solution is provided at 25 µL, 10mM.
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ZM 306416 is a selective inhibitor of VEGFR with IC50 value of 0.67μM [1]. It is also reported that ZM 306416 inhibits EGFR with IC50 value less than 10 nM [2].
Vascular endothelial growth factor receptor (VEGFR) is a key element of the extracellular matrix(ECM) and plays an important role in angiogenesis cooperating with its ligand VEGF. Several studies have demonstrated that VEGFRs expressed in liquid and solid tumor cells, such as NSCLC, melanoma, prostate cancer, leukemia, mesothelioma, and breast cancer and are being regarded as a promising target in clinical [3].
ZM 306416 is a potent VEGFR inhibitor and has a different selectivity with other reported VEGFR inhibitors. Using A549-EGFRB cells for EGFRB assay revealed that ZM 306416 exhibited inhibitory activity on VEGFR with IC50 value of 670 nM [1]. When tested with human thyroid follicular cells, ZM 306416 treatment exhibited function on reducing VEGFR2 phosphorylation and inhibiting endogenous, steady-state levels of p42/44 MAPK phosphorylation [4].
References:
1. Antczak, C., et al., A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen, 2012. 17(7): p. 885-99.
2. Choi KJ, Baik IH, Ye SK et al. Molecular Targeted Therapy for Hepatocellular Carcinoma: Present Status and Future Directions. Biol Pharm Bull. 2015;38(7):986-91.
3. Choi, K.J., et al., Molecular Targeted Therapy for Hepatocellular Carcinoma: Present Status and Future Directions. Biol Pharm Bull, 2015. 38(7): p. 986-91.
4. Susarla, R., J.C. Watkinson, and M.C. Eggo, Regulation of human thyroid follicular cell function by inhibition of vascular endothelial growth factor receptor signalling. Mol Cell Endocrinol, 2012. 351(2): p. 199-207.
| Cas No. | 690206-97-4 | SDF | |
| 同義語 | CB-676475 | ||
| Chemical Name | N-(4-chloro-2-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine | ||
| Canonical SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=C(C=C3)Cl)F)OC | ||
| Formula | C16H13ClFN3O2 | M.Wt | 333.74 |
| 溶解度 | ≥ 33.4mg/mL in DMSO | 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 | 2.9963 mL | 14.9817 mL | 29.9634 mL |
| 5 mM | 599.3 μL | 2.9963 mL | 5.9927 mL |
| 10 mM | 299.6 μL | 1.4982 mL | 2.9963 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)