Antibodies
ZM 306416
- 貨號 Cat. No.
- S2897
- 規格 Size
- 10mgã€10mM/1mL
- 品牌 Brand
- Selleckchem
Description
ZM 306416
Catalog No.S2897
ZM 306416 is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | ZM 306416 is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM. | |||||
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| Targets | Src | VEGFR1 | Abl | |||
| IC50 | 0.33 μM | 0.33 μM | 1.3 μM [1] | |||
| In vitro | 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. [1] ZM-306416 significantly inhibits the ERRα assay with IC50 of 7.3 μM in the GeneBLAzer T-Rex RORγ-UAS-bla HEK293T cell line. [2] 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. [3] ZM306416 (1 μM) enhances follicle formation and decreased nuclear distribution in human thyroid follicular cells. [4] | |||||
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Protocol(Only for Reference)
Kinase Assay: [1]
| Binding assay | The potency of ZM-306416 is measured in dose-response studies in a 384-well format using 12 doubling dilutions in duplicate with a 10 µM and 1 µM ZM-306416 concentration as the upper limit. All reagents transfers are performed using the PP-384-M Personal Pipettor. ZM-306416 or controls are added to the wells at a volume of 1 µL to white 384-well microplates. Controls consisted of 1% DMSO (v/v) (high control) and 30 µM staurosporine in 1% DMSO (v/v) (low controls). The assay buffer is 25 mM HEPES/NaOH (pH 7.5) and contained 10 mM MgCl2, 2 mM TCEP, 20 mM β-glycerol phosphate, and 100 µM Na3VO4; for each kinase on the panel, 4 µL kinase dilution in assay buffer is added to the wells to reach a final concentration of 50 nM enzyme. After enzyme addition, kinase and ZM-306416 are preincubated for 10 min at room temperature. Then, 5 µL of a mix containing ATP and Poly(Glu, Tyr) substrates in solution in assay buffer is added to the wells to reach a final concentration of 200 礛. After a 45 min reaction at room temperature, 10 礚 ADP-Glo Reagent is added to each well. After a 40-min incubation, 20 礚 Kinase Detection Reagent is added followed by a 60-min incubation. The luminescence signal output is measured on the LEADseeker multimodality imaging system. |
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References
Chemical Information
| Molecular Weight (MW) | 333.74 |
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| Formula | C16H13ClFN3O2 |
| CAS No. | 690206-97-4 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 67 mg/mL (200 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 4-Quinazolinamine, N-(4-chloro-2-fluorophenyl)-6,7-dimethoxy- |
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