ZM 306416

VEGFR (Flt and KDR) inhibitor CAS# 690206-97-4

ZM 306416

Catalog No. BCC3964----Order now to get a substantial discount!

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Chemical structure

ZM 306416

3D structure

Chemical Properties of ZM 306416

Cas No. 690206-97-4 SDF Download SDF
PubChem ID 5329006 Appearance Powder
Formula C16H13ClFN3O2 M.Wt 333.74
Type of Compound N/A Storage Desiccate at -20°C
Synonyms CB 676475
Solubility DMSO : 50 mg/mL (149.82 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name N-(4-chloro-2-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine
SMILES COC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=C(C=C3)Cl)F)OC
Standard InChIKey YHUIUSRCUKUUQA-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H13ClFN3O2/c1-22-14-6-10-13(7-15(14)23-2)19-8-20-16(10)21-12-4-3-9(17)5-11(12)18/h3-8H,1-2H3,(H,19,20,21)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ZM 306416

DescriptionZM 306416 is an inhibitor of VEGFR (Flt and KDR) with an IC50 value of 0.33 μM for VEGFR1.
TargetsVEGFR1SrcAbl   
IC500.33 μM0.33 μM1.3 μM    

ZM 306416 Dilution Calculator

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ZM 306416 Molarity Calculator

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Preparing Stock Solutions of ZM 306416

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9963 mL 14.9817 mL 29.9634 mL 59.9269 mL 74.9086 mL
5 mM 0.5993 mL 2.9963 mL 5.9927 mL 11.9854 mL 14.9817 mL
10 mM 0.2996 mL 1.4982 mL 2.9963 mL 5.9927 mL 7.4909 mL
50 mM 0.0599 mL 0.2996 mL 0.5993 mL 1.1985 mL 1.4982 mL
100 mM 0.03 mL 0.1498 mL 0.2996 mL 0.5993 mL 0.7491 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on ZM 306416

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.

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References on ZM 306416

Low nitrogen stress stimulating the indole-3-acetic acid biosynthesis of Serratia sp. ZM is vital for the survival of the bacterium and its plant growth-promoting characteristic.[Pubmed:27803972]

Arch Microbiol. 2017 Apr;199(3):425-432.

Serratia sp. ZM is a plant growth-promoting (PGP) bacterial strain isolated from the rhizospheric soil of Populus euphratica in northwestern China. In this study, low nitrogen supply significantly stimulated the production of indole-3-acetic acid (IAA) in Serratia sp.ZM. The inoculation of the bacterium to wheat seedlings improved plant growth compared with the uninoculated group, and the stimulating effect was more prominent under low nitrogen stress. Inactivation of the predicted key gene in the IAA biosynthesis pathway impaired IAA production and significantly hampered mutant growth in poor medium. Furthermore, the IAA-deficient mutant lost the PGP effect under either normal or low nitrogen conditions in plant experiments. This study revealed the significant impact of environmental nitrogen levels on IAA production in the PGP strain and the vital effect of IAA on resistance physiology of both the bacterium and host plant. The characteristics of Serratia sp. ZM also indicated its application potential as a biofertilizer for plants, especially those suffering from poor nitrogen soil.

ZM-66, a new podophyllotoxin derivative inhibits proliferation and induces apoptosis in K562/ADM cells.[Pubmed:25264886]

Chin Med Sci J. 2014 Sep;29(3):174-9.

OBJECTIVE: To investigate the anti-tumor effect of ZM-66 on multidrug-resistant leukemic cell line K562/ADM. METHODS: The K562/ADM cells were treated with varying concentrations (0, 1, 2, 4 x 10(-)(3) mmol/L) of ZM-66 or etoposide for 24 hours. The proliferation was detected by Sulforhodamine B Sodium Salt (SRB) assay and apoptosis was detected by flow cytometry analysis and fluorescent staining. In addition, the expression levels of p53 and bax genes in K562/ADM cells were detected by RT-PCR analysis. The level of P-glycoprotein (P-gp), P53 and Bax protein in K562/ADM cells were detected by Western blot assay. RESULTS: SRB assay demonstrated that etoposide had little inhibitory effect on K562/ADM cells, whereas ZM-66 (1, 2, 4 x 10(-)(3) mmol/L) had significantly inhibitory effect on K562/ADM cells (all P<0.01). The acridine orange/propidium iodide dual staining showed that there were typical condensation of chromatin and nuclear fragmentation nuclei with red color in ZM-66 treated cells. Flow cytometric analysis showed that there was a significantly increase of apoptotic cells in K562/ADM cells after treated with ZM-66. RT-PCR showed that the p53 and bax mRNA expression levels in K562/ADM cells treated with ZM-66 at 1, 2, 4 x 10(-)(3) mmol/L were higher than those in the cell without treatment. Western blot showed that the P53 and Bax protein expression levels in K562/ADM cells treated with ZM-66 at 2, 4 x 10(-)(3) mmol/L were higher than those in the cell without treatment. But the P-gp protein expression level in K562/ADM cells treated with ZM-66 at 2, 4 x 10(-)(3) mmol/L was gradually lower than those in the cell without treatment. CONCLUSION: ZM-66 is able to induce cell death by apoptosis in vitro, as a result of the reverse of the apoptosis resistance in drug-resistant K562/ADM cells by modulating expression of key factors associated with apoptosis induction.

[New metalloendopeptidase of Morganella morganii ZM].[Pubmed:25895364]

Bioorg Khim. 2014 Nov-Dec;40(6):682-7.

Proteolytic activity which is inhibited in the presence of o-phenanthroline was found in M. morganii ZM. Intracellular proteases of M. morganii ZM unlimited split musculoskeletal actin in contrast to grimelysin. Several proteolitic proteins of M. morganii ZM cells were identified by zymography with gelatin. Metalloproteinase of M. morganii ZM cell lysate was purified by hydrophobic chromatography fractionation. The molecular weight of the protein was 35 kDa.

Description

ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.

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