Name | ZM 306416 |
Synonyms | CB676475 CB-676475 CB 676475 ZM 306416 ZM 306416 HYDROCHLORIDE 4-QuinazolinaMine,N-(4-chloro-2-fluorophenyl)-6,7-diMethoxy- 4-[(4'-CHLORO-2'-FLUORO)PHENYLAMINO]-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE ZM 213689 DisodiuM Salt (MeropeneM iMpurity) (Mixture of double bond isoMers) |
CAS | 690206-97-4 |
Molecular Formula | C16H13ClFN3O2 |
Molar Mass | 333.74 |
Melting Point | >161°C (dec.) |
Solubility | DMSO : 50 mg/mL (149.82 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) |
Appearance | Off-white solid. |
Color | Light Orange to Brown |
Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
Stability | Hygroscopic |
Use | ZM-306416 (CB 676475) is an effective inhibitor of VEGFR, with IC50 values of 0.1 and 2 μM for KDR and Flt respectively. ZM-306416 is also an inhibitor of EGFR, with an IC50 value of less than 10 nM. |
In vitro study | ZM-306416, selective antiproliferative effects were induced by action on EGFR-Tropic NSCLC cell lines H3255 and HCC4011 with IC50 of 0.09 μm and 0.072 μm, respectively. ZM-306416 inhibition of particle formation, IC50 0.67 μm. ZM-306416, the cell line GeneBLAzer T-Rex RORγ-UAS-bla HEK293T significantly inhibited ERRα detection with IC50 of 7.3 μm. ZM306416 (300 nM) acts on human thyroid follicular cells, completely inhibits PAA secretion and stimulates [125I] uptake, and abrogates pVEGFR2 (Y1214) expression. ZM306416 (< 10 μm) significantly inhibited the steady-state phosphorylation of p42/44 MAPK, but did not affect the expression of the non-phosphorylated form. ZM306416(3 μm) significantly increased cell death in human thyroid follicular cells. ZM306416 weakly inhibited VEGF secretion and increased PlGF production. ZM306416(1 μm) acts on human thyroid follicular cells to increase follicle formation and reduce nuclear distribution. ZM-306416 induced a selective anti-proliferative effect with IC50 of 0.09 μm and 0.072 μm on the EGFR-Tropic NSCLC cell lines H3255 and HCC4011, respectively. ZM-306416 inhibition of particle formation, IC50 0.67 μm. ZM-306416, the cell line GeneBLAzer T-Rex RORγ-UAS-bla HEK293T significantly inhibited ERRα detection with IC50 of 7.3 μm. ZM306416 (300 nM) acts on human thyroid follicular cells, completely inhibits PAA secretion, and stimulates [ZM306416(1 μm) to act on human thyroid follicular cells, increasing follicle formation and reducing nuclear distribution. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.996 ml | 14.982 ml | 29.963 ml |
5 mM | 0.599 ml | 2.996 ml | 5.993 ml |
10 mM | 0.3 ml | 1.498 ml | 2.996 ml |
5 mM | 0.06 ml | 0.3 ml | 0.599 ml |
biological activity | ZM 306416 is a VEGFR(Flt and KDR) inhibitor that acts on VEGFR1, the IC50 was 0.33 μm and also inhibited EGFR with an IC50 of <10 nM. ZM 306416 (CB 676475) is a VEGFR(Flt and KDR) inhibitor that acts on VEGFR1 with an IC50 of 0.33 μm and also inhibits EGFR with an IC50 of <10 nM. |
in vitro study | ZM-306416 induces selective antiproliferative effects on EGFR-addicted NSCLC cell lines H3255 and HCC4011, the IC50 values were 0.09 μm and 0.072 μm, respectively. ZM-306416 inhibition of particle formation, IC50 0.67 μm. ZM-306416, the cell line GeneBLAzer T-Rex RORγ-UAS-bla HEK293T significantly inhibited ERRα detection with IC50 of 7.3 μm. ZM306416 (300 nM) acts on human thyroid follicular cells, completely inhibits PAA secretion and stimulates [125I] uptake, and abrogates pVEGFR2 (Y1214) expression. ZM306416 (< 10 μm) significantly inhibited the steady-state phosphorylation of p42/44 MAPK, but did not affect the expression of the non-phosphorylated form. ZM306416(3 μm) significantly increased cell death in human thyroid follicular cells. ZM306416 weakly inhibited VEGF secretion and increased PlGF production. ZM306416(1 μm) acts on human thyroid follicular cells to increase follicle formation and reduce nuclear distribution. ZM-306416 induced a selective anti-proliferative effect with IC50 of 0.09 μm and 0.072 μm on the EGFR-Tropic NSCLC cell lines H3255 and HCC4011, respectively. ZM-306416 inhibition of particle formation, IC50 0.67 μm. ZM-306416, the cell line GeneBLAzer T-Rex RORγ-UAS-bla HEK293T significantly inhibited ERRα detection with IC50 of 7.3 μm. ZM306416 (300 nM) acts on human thyroid follicular cells, completely inhibits PAA secretion, and stimulates [ZM306416(1 μm) to act on human thyroid follicular cells, increasing follicle formation and reducing nuclear distribution. |
Target | TargetValue VEGFR1 0.33 μm Src 0.33 μm Abl 1.3 μm |
Target | Value |
VEGFR1 | 0.33 μM |
Src | 0.33 μM |
Abl | 1.3 μM |