N-[[[3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-benzeneacetamide
MGCD-265
CAS: 875337-44-3
Molecular Formula: C26H20FN5O2S2
N-[[[3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-benzeneacetamide - Names and Identifiers
N-[[[3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-benzeneacetamide - Physico-chemical Properties
| Molecular Formula | C26H20FN5O2S2 |
| Molar Mass | 517.6 |
| Density | 1.41 |
| pKa | 10.07±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | MGCD-265 is a multi-target receptor tyrosine kinase inhibitor. MGCD-265 effectively inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2 with an IC50 of 1 nM to 7 nM. MGCD-265 acts on c-Met-driven tumor cells (MKN45, MNNG-HOS, and SNU-5) and non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), inhibiting cell proliferation, the IC50 values were 6 nM-30 nM and 1 μM-3 μm, respectively. The 40 nM-5 μm MGCD-265 effect on serum-starved MKN45 cells effectively inhibited c-Met of phosphorylation and c-Met of downstream signaling pathways including Erk, Akt, Stat3, and Fak. 6 nM-1 M MGCD-265 in MKN45 cells, also induced apoptosis. MGCD-265 is a multi-target receptor tyrosine kinase inhibitor. MGCD-265 effectively inhibited Met and MetMGCD-265 acted on tumor cells driven by c-Met (MKN45, MNNG-HOS, And SNU-5) and non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), inhibit cell proliferation with IC50 of 6 nM-30 nM and 1 μM-3 μm, respectively. The 40 nM-5 μm MGCD-265 effect on serum-starved MKN45 cells effectively inhibited c-Met of phosphorylation and c-Met of downstream signaling pathways including Erk, Akt, Stat3, and Fak. 6 nM-1 M MGCD-265 in MKN45 cells, also induced apoptosis. |
| In vivo study | MGCD-265 dosed from 20 mg/kg to 60 mg/kg in c-Met-driven or not c-Met-driven mice bearing MKN45, U87MG, MDA-MB-231, COLO205, and A549 xenografts, inhibits tumor growth and c-Met signaling pathway. MGCD-265 at a dose of 40 mg/kg acts on the tumor and plasma of mice bearing U87MG xenografts, and also down-regulates genes related to angiogenesis, including VEGF and IL-8. MGCD-265 also inhibited the plasma concentration by c-Met. MGCD-265 dosed from 20 mg/kg to 60 mg/kg in c-Met-driven or not c-Met-driven mice bearing MKN45, U87MG, MDA-MB-231, COLO205, and A549 xenografts, inhibits tumor growth and c-Met signaling pathway. MGCD-265 at a dose of 40 mg/kg acts on the tumor and plasma of mice bearing U87MG xenografts, and also down-regulates genes related to angiogenesis, including VEGF and IL-8. MGCD-265 also inhibited the plasma concentration by c-Met. |
N-[[[3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-benzeneacetamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.932 ml | 9.66 ml | 19.32 ml |
| 5 mM | 0.386 ml | 1.932 ml | 3.864 ml |
| 10 mM | 0.193 ml | 0.966 ml | 1.932 ml |
| 5 mM | 0.039 ml | 0.193 ml | 0.386 ml |
Last Update：2024-01-02 23:10:35
N-[[[3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-benzeneacetamide - Reference Information
| biological activity | MGCD-265 is an effective, and ATP competitive c-Met and VEGFR1/2/3 inhibitors with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively, also inhibit Ron and tie2. Phase 1/2. MGCD-265 is a potent, multitargeted, and ATP-competitive c-Met and VEGFR1/2/3 inhibitor with an IC50 of 1 nM, 3 nM/3 nM/4 nM, also inhibited Ron and tie2. Phase 1/2. |
| in vitro study | MGCD-265 is a multi-target receptor tyrosine kinase inhibitor. MGCD-265 effectively inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2 with an IC50 of 1 nM to 7 nM. MGCD-265 acts on c-Met-driven tumor cells (MKN45, MNNG-HOS, and SNU-5) and non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), inhibiting cell proliferation, the IC50 values were 6 nM-30 nM and 1 μM-3 μm, respectively. The 40 nM-5 μm MGCD-265 effect on serum-starved MKN45 cells effectively inhibited c-Met of phosphorylation and c-Met of downstream signaling pathways including Erk, Akt, Stat3, and Fak. 6 nM-1 M MGCD-265 in MKN45 cells, also induced apoptosis. MGCD-265 is a multi-target receptor tyrosine kinase inhibitor. MGCD-265 effectively inhibited Met and MetMGCD-265 acted on tumor cells driven by c-Met (MKN45, MNNG-HOS, And SNU-5) and non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), inhibit cell proliferation with IC50 of 6 nM-30 nM and 1 μM-3 μm, respectively. The 40 nM-5 μm MGCD-265 effect on serum-starved MKN45 cells effectively inhibited c-Met of phosphorylation and c-Met of downstream signaling pathways including Erk, Akt, Stat3, and Fak. 6 nM-1 M MGCD-265 in MKN45 cells, also induced apoptosis. |
| in vivo study | MGCD-265 at a dose of 20 mg/kg-60 mg/kg for c-Met-driven or non-c-Met-driven carriers of MKN45, U87MG, MDA-MB-231, COLO205, and A549 xenografts in mice, inhibited tumor growth and c-Met signaling pathway. MGCD-265 at a dose of 40 mg/kg acts on the tumor and plasma of mice bearing U87MG xenografts, and also down-regulates genes related to angiogenesis, including VEGF and IL-8. MGCD-265 also inhibited the plasma concentration by c-Met. MGCD-265 dosed from 20 mg/kg to 60 mg/kg in c-Met-driven or not c-Met-driven mice bearing MKN45, U87MG, MDA-MB-231, COLO205, and A549 xenografts, inhibits tumor growth and c-Met signaling pathway. MGCD-265 at a dose of 40 mg/kg acts on the tumor and plasma of mice bearing U87MG xenografts, and also down-regulates genes related to angiogenesis, including VEGF and IL-8. MGCD-265 also inhibited the plasma concentration by c-Met. |
| characteristics | MGCD-265 is a potent multi-target ATP competitive receptor tyrosine kinase inhibitor, including Met, VEGFR, Ron, and tie2. |
| Target | TargetValue Met 1 nM RON 2 nM VEGFR1 3 nM VEGFR2 3 nM VEGFR3 4 nM |
| Target | Value |
| Met | 1 nM |
| RON | 2 nM |
| VEGFR1 | 3 nM |
| VEGFR2 | 3 nM |
| VEGFR3 | 4 nM |
Last Update：2024-04-09 20:02:46
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Product Name: MGCD-265 Visit Supplier Webpage Request for quotation
CAS: 875337-44-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 875337-44-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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