product name ZM 306416
Description: ZM 306416 (also known as CB 676475) is a potent inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM. Using A549-EGFRB cells for EGFRB assay revealed that ZM 306416 exhibited inhibitory activity on VEGFR with IC50 value of 670 nM. 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.
References: J Biomol Screen. 2012 Aug;17(7):885-99; Mol Cell Endocrinol. 2012 Apr 4;351(2):199-207; J Cell Physiol. 2012 May;227(5):1992-2002.
333.74
Formula
C16H13ClFN3O2
CAS No.
690206-97-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 67 mg/mL (200.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
CB 676475
other peoduct :
| In Vitro |
In vitro activity: ZM-306416 induces selective antiproliferative effect toward the EGFR-addicted NSCLC cell lines H3255 and HCC4011 with IC50 of 0.09 µM and 0.072 µM, respectively. ZM-306416 inhibits granule formation with IC50 of 0.67 μM. ZM-306416 significantly inhibits the ERRα assay with IC50 of 7.3 μM in the GeneBLAzer T-Rex RORγ-UAS-bla HEK293T cell line. ZM306416 (300 nM) completely inhibits PAA secretion and stimulates [125]I uptake in human thyroid follicular cells. ZM306416 (300 nM) abolishes pVEGFR2 (Y1214) expression in human thyroid follicular cells. ZM306416 (< 10 μM) has marked inhibitory effects on the steady state phosphorylation of p42/44 MAPK but does not affect the expression of the unphosphorylated form. ZM306416 (3 μM) significantly increases cell death in human thyroid follicular cells. ZM306416 (3 μM) significantly increases cell death in human thyroid follicular cells. ZM306416 weakly inhibits the secretion of VEGF and increases the production of PlGF. ZM306416 (1 μM) enhances follicle formation and decreased nuclear distribution in human thyroid follicular cells. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Biomol Screen. 2012 Aug;17(7):885-99; Mol Cell Endocrinol. 2012 Apr 4;351(2):199-207; J Cell Physiol. 2012 May;227(5):1992-2002. |
