VEGFR2/C-RAF kinase-IN-1
VEGFR2/C-RAF kinase-IN-1 is a type II dual kinase inhibitor targeting VEGFR2 and C-RAF, with IC50 values of 12.22 nM and 38.04 nM, respectively. VEGFR2/C-RAF kinase-IN-1 binds VEGFR2 and CRAF in a Type-II mode and inhibits the downstream Raf-MEK-ERK signaling cascade. VEGFR2/C-RAF kinase-IN-1 induces cell cycle arrest, apoptosis, and intracellular ROS accumulation in H1299 cells, while partially inhibiting P-gp efflux function. VEGFR2/C-RAF kinase-IN-1 can be used for cancer research, such as non-small cell lung cancer and liver cancer.
For research use only. We do not sell to patients.
- Formula: C30H27ClF3N5O4S
- Molecular Weight:646.08
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
VEGFR2 12.22 nM (IC50) |
C-Raf 38.04 nM (IC50) |
MEK |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | IC50 |
8.40 μM
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Inhibition of Huh7 cell viability incubated for 48 hrs by CCK-8 assay.
Inhibition of Huh7 cell viability incubated for 48 hrs by CCK-8 assay.
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42594418 |
| HepG2 | IC50 |
9.95 μM
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Inhibition of HepG2 cell viability incubated for 48 hrs by CCK-8 assay.
Inhibition of HepG2 cell viability incubated for 48 hrs by CCK-8 assay.
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42594418 |
| NCI-H1299 | IC50 |
8.32 μM
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Inhibition of H1299 cell viability incubated for 48 hrs by CCK-8 assay.
Inhibition of H1299 cell viability incubated for 48 hrs by CCK-8 assay.
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42594418 |
| HeLa | IC50 |
11.47 μM
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Inhibition of HeLa cell viability incubated for 48 hrs by CCK-8 assay.
Inhibition of HeLa cell viability incubated for 48 hrs by CCK-8 assay.
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42594418 |
| SW480 | IC50 |
22.65 μM
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Inhibition of SW480 cell viability incubated for 48 hrs by CCK-8 assay.
Inhibition of SW480 cell viability incubated for 48 hrs by CCK-8 assay.
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42594418 |
| THLE-2 | IC50 |
12.73 μM
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Inhibition of THLE-2 cell viability incubated for 48 hrs by CCK-8 assay.
Inhibition of THLE-2 cell viability incubated for 48 hrs by CCK-8 assay.
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42594418 |
In Vitro
VEGFR2/C-RAF kinase-IN-1 (compound 5J) (10 μM; 48 h) exhibits broad-spectrum in vitro anticancer activity with acceptable tumor selectivity[1].
VEGFR2/C-RAF kinase-IN-1 (2.5-10 μM; 24-48 h) inhibits H1299 cell migration in a dose- and time-dependent manner[1].
VEGFR2/C-RAF kinase-IN-1 (2.5-10 μM; 7-14 days) effectively inhibits the long-term proliferative capacity of H1299 cells[1].
VEGFR2/C-RAF kinase-IN-1 is a potent inhibitor of VEGFR2 and CRAF in cell-free kinase assays, with IC50 values of 12.22 nM and 38.04 nM, respectively[1].
VEGFR2/C-RAF kinase-IN-1 (2.5-20 μM; 1 h) may partially interfere with P-gp-mediated efflux in H1299 cells[1].
VEGFR2/C-RAF kinase-IN-1 (2.5-10 μM; 48 h) effectively inhibits Raf-MEK-ERK signaling in H1299 cells[1].
VEGFR2/C-RAF kinase-IN-1 (2.5-20 μM; 48 h) inhibits H1299 cell proliferation mainly through G0/G1 phase arrest; induces apoptosis in H1299 cells; and effectively triggers oxidative stress in H1299 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh7, HepG2, H1299, HeLa, SW480, and THLE-2
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Concentration:5, 10, 15, 20, 30 μM
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Incubation Time:48 h
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Result:Exhibits broad-spectrum in vitro anticancer activity.
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Cell Line:H1299
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Concentration:2.5, 5, 10 μM
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Incubation Time:0, 24, 48 h
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Result:Inhibited H1299 cell migration.
Wound closure rates dropped to 21.88% (24 h) and 58.71% (48 h) at 2.5 μM, decreased to 16.28% (24 h) and 46.96% (48 h) at 5 μM, and were restricted to 12.74% (24 h) and 34.19% (48 h) at 10 μM.
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Cell Line:H1299
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Concentration:2.5, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Induced a dose-dependent alteration in cell cycle distribution.
At 2.5-10 μM, caused progressive G0/G1 phase arrest, with the population increasing from 60.59% to 73.63% (2.5 μM), 82.39% (5 μM), and 85.10% (10 μM).
At 20 μM, a biphasic response emerged with a significant accumulation of cells in the G2/M phase (28.85%).
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Cell Line:H1299
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Concentration:2.5, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Significantly induced apoptosis in H1299 cells in a concentration-dependent manner.
At 2.5 μM, a slight increase in early apoptotic cells was observed.
With increasing concentrations (5-20 μM), both early and late apoptotic cell populations progressively increased, with late apoptosis reaching approximately 4.86% at 20 μM.
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Cell Line:H1299
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Concentration:2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Suppressed the activation of the Raf-MEK-ERK pathway in a dose-dependent manner.
The relative p-MEK/MEK ratio decreased from 1.00 in the vehicle control to 1.07, 0.45, and 0.28 at 2.5, 5, and 10 μM, respectively.
Concurrently, the p-ERK/ERK ratio showed a progressive decline, decreasing to 0.70, 0.48, and 0.32 at the same concentrations.
Chemical Information
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Molecular Weight 646.08
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Formula C30H27ClF3N5O4S
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SMILES
ClC1=CC=C(NC(NC2=CC(C3=CSC(NC(CN4CCC5=CC(OC)=C(OC)C=C5C4)=O)=N3)=CC=C2)=O)C=C1C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VEGFR2/C-RAF kinase-IN-1 Related Classifications
HY-189471 Related Classifications
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