VEGFR/PDGFR-IN-2
VEGFR/PDGFR-IN-2 is a VEGFR1/2/3, PDGFRα/β, and Tie-2 tyrosine kinase inhibitor. VEGFR/PDGFR-IN-2 inhibits endothelial tube formation and endothelial migration by blocking VEGF-induced receptor phosphorylation and PDGF-BB signaling, reduces tumor microvessel density, pericyte recruitment, and tumor interstitial fluid pressure, and enhances the antitumor activity of CPT-11. VEGFR/PDGFR-IN-2 can be used for research on solid tumors.
For research use only. We do not sell to patients.
- CAS No.: 919279-04-2
- Formula: C21H15F4N5O2
- Molecular Weight:445.38
-
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]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
All VEGFR Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
VEGFR1 |
VEGFR2 |
VEGFR3 |
PDGFRα |
PDGFRβ |
Tie2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
2.5 nM
|
Inhibition of VEGF-induced VEGFR2 phosphorylation in HUVECs after 2 hrs incubation with VEGFR/PDGFR-IN-2 and 5 mins stimulation with VEGF measured by Western blotting.
Inhibition of VEGF-induced VEGFR2 phosphorylation in HUVECs after 2 hrs incubation with VEGFR/PDGFR-IN-2 and 5 mins stimulation with VEGF measured by Western blotting.
|
22320850 |
| HUVEC | IC50 |
2.8 nM
|
Inhibition of VEGF-stimulated proliferation of HUVECs incubated with VEGFR/PDGFR-IN-2 for 5 days assessed by Cell Counting Kit-8.
Inhibition of VEGF-stimulated proliferation of HUVECs incubated with VEGFR/PDGFR-IN-2 for 5 days assessed by Cell Counting Kit-8.
|
22320850 |
| HUVEC | IC50 |
3.3 nM
|
Inhibition of VEGF-induced tube formation in HUVECs cocultured with normal human dermal fibroblasts incubated with VEGFR/PDGFR-IN-2 for 7 days assessed by CD31 staining and fluoroscopic imaging.
Inhibition of VEGF-induced tube formation in HUVECs cocultured with normal human dermal fibroblasts incubated with VEGFR/PDGFR-IN-2 for 7 days assessed by CD31 staining and fluoroscopic imaging.
|
22320850 |
In Vitro
VEGFR/PDGFR-IN-2 (0.064-200 nM; 2 h) inhibits VEGF-induced VEGFR2 phosphorylation in HUVECs and PDGF-BB-induced PDGFRβ phosphorylation in CASMCs, with IC50 values of 2.5 and 3.6 nM, respectively[1].
VEGFR/PDGFR-IN-2 (5 days) inhibits VEGF-stimulated HUVEC proliferation with an IC50 of 2.8 nM[1].
VEGFR/PDGFR-IN-2 (6 days) inhibits PDGF-BB-stimulated CASMC proliferation with an IC50 of 9.6 nM[1].
VEGFR/PDGFR-IN-2 (0.3-10 nM; 7 days) inhibits VEGF-induced tube formation in HUVECs co-cultured with normal human dermal fibroblasts, with an IC50 of 3.3 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HUVECs and CASMCs
-
Concentration:0.064, 0.32, 1.6, 8.0, 40, 200 nM
-
Incubation Time:2 h (pretreatment)
-
Result:Inhibited VEGF-induced VEGFR2 phosphorylation in HUVECs with an IC50 of 2.5 nM.
Inhibited PDGF-BB-induced PDGFRβ phosphorylation in CASMCs with an IC50 of 3.6 nM.
In Vivo
VEGFR/PDGFR-IN-2 (1.5-5.0 mg/kg; oral; twice daily; days 2-21) inhibits HT-29 tumor growth and reduces tumor interstitial fluid pressure, enhancing intratumoral uptake of CPT-11 and its active metabolite SN-38[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:athymic nude (BALB/cA Jcl-nu/nu; 6-8 weeks old)[1]
-
Dosage:1.5, 6 mg/kg (7 days); 1.5, 6 mg/kg (21 days); 3, 10 mg/kg (3 days)
-
Administration:p.o. twice daily for 7 and 21 days; p.o. once daily for 3 days
-
Result:Showed a T/C ratio of 59% at 1.5 mg/kg p.o. twice daily for 7 days.
Produced tumor stasis with a T/C ratio of 5% at 6 mg/kg p.o. twice daily for 7 days.
Showed a T/C ratio of 39% at 1.5 mg/kg p.o. twice daily for 21 days.
Showed a T/C ratio of 4% at 6.0 mg/kg p.o. twice daily for 21 days.
Reduced tumor microvessel density (CD31-positive filaments) and pericyte recruitment to tumor blood vessels in a dose-dependent manner.
-
Animal Model:athymic nude (BALB/cA Jcl-nu/nu)[1]
-
Dosage:1.5 mg/kg (2 weeks); 1.5 mg/kg (21 days); 5.0 mg/kg (21 days); 1.5 mg/kg + CPT-11 30 mg/kg (every 3 days for 2 weeks); 1.5 mg/kg + CPT-11 30 mg/kg (Days 2, 4, 7, or 14)
-
Administration:p.o. twice daily for 2 weeks; p.o. twice daily for 21 days; p.o. twice daily with i.p. every 3 days for 2 weeks; p.o. twice daily with i.p. on Days 2, 4, 7, or 14
-
Result:Showed a T/C ratio of 58% at 1.5 mg/kg p.o. twice daily for 2 weeks.
Produced a T/C ratio of 35% with CPT-11 plus comp.20d.
Showed a T/C ratio of 44% at 1.5 mg/kg p.o. twice daily for 21 days.
Showed a T/C ratio of 16% at 5.0 mg/kg p.o. twice daily for 21 days.
Decreased tumor interstitial fluid pressure by 49%, 55%, 46%, and 38% on Days 2, 4, 8, and 15, respectively, compared with vehicle.
Increased tumor tissue SN-38 concentration on Day 4, Day 7, and Day 14.
Showed no significant differences in plasma SN-38 concentrations between control and comp.20d groups.
Chemical Information
-
CAS No. 919279-04-2
-
Molecular Weight 445.38
-
Formula C21H15F4N5O2
-
SMILES
O=C(NC1=CC=CC(=C1)C(F)(F)F)NC2=CC=C(OC3=NC=NC=4C=CN(C34)C)C=C2F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)
VEGFR/PDGFR-IN-2 Related Classifications
HY-18180 Related Classifications
Powered by Bioz