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ZM 306416

Catalog No.
A8684
VEGFR (Flt and KDR) inhibitor
Grouped product items
SizePriceStock Qty
10mg
$83.00
In stock
50mg
$289.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt333.74
Cas No.690206-97-4
FormulaC16H13ClFN3O2
Solubility≥33.4 mg/mL in DMSO; insoluble in H2O; ≥2.85 mg/mL in EtOH with gentle warming
Chemical NameN-(4-chloro-2-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine
SDFDownload SDF
Canonical SMILESCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=C(C=C3)Cl)F)OC
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description ZM 306416 is an inhibitor of VEGFR (Flt and KDR) with an IC50 value of 0.33 μM for VEGFR1.
Targets VEGFR1 Src Abl      
IC50 0.33 μM 0.33 μM 1.3 μM      

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