1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. VEGFR-2-IN-30

VEGFR-2-IN-30 is a VEGFR-2 inhibitor (IC50: 66 nM). VEGFR-2-IN-30 also inhibits PDGFR, EGFR and FGFR1 with IC50s of 180, 98, 82 nM respectively. VEGFR-2-IN-30 arrests cancer cell at S-phase and induces early and late apoptosis.

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VEGFR-2-IN-30

VEGFR-2-IN-30 Chemical Structure

CAS No. : 3037960-64-5

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Description

VEGFR-2-IN-30 is a VEGFR-2 inhibitor (IC50: 66 nM). VEGFR-2-IN-30 also inhibits PDGFR, EGFR and FGFR1 with IC50s of 180, 98, 82 nM respectively. VEGFR-2-IN-30 arrests cancer cell at S-phase and induces early and late apoptosis[1].

IC50 & Target[1]

VEGFR2

66 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
RPTEC IC50
48.33 3
Compound: 8f
Cytotoxicity against human RPTEC cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
Cytotoxicity against human RPTEC cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
[PMID: 36395650]
UO-31 IC50
5.29 3
Compound: 8f
Cytotoxicity against human UO-31 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
Cytotoxicity against human UO-31 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
[PMID: 36395650]
UO-31 IC50
4.52 3
Compound: 8f
Cytotoxicity against human UO-31 cells assessed as inhibition of cell growth preincubated for 2 hrs followed by administration of single dose of 8 Gy gamma irradiation for 21.4 mins and measured 24 hrs after irradiation by MTT assay
Cytotoxicity against human UO-31 cells assessed as inhibition of cell growth preincubated for 2 hrs followed by administration of single dose of 8 Gy gamma irradiation for 21.4 mins and measured 24 hrs after irradiation by MTT assay
[PMID: 36395650]
RPTEC IC50
48.33 3
Compound: 8f
Cytotoxicity against human RPTEC cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
Cytotoxicity against human RPTEC cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
[PMID: 36395650]
UO-31 IC50
4.52 3
Compound: 8f
Cytotoxicity against human UO-31 cells assessed as inhibition of cell growth preincubated for 2 hrs followed by administration of single dose of 8 Gy gamma irradiation for 21.4 mins and measured 24 hrs after irradiation by MTT assay
Cytotoxicity against human UO-31 cells assessed as inhibition of cell growth preincubated for 2 hrs followed by administration of single dose of 8 Gy gamma irradiation for 21.4 mins and measured 24 hrs after irradiation by MTT assay
[PMID: 36395650]
UO-31 IC50
5.29 3
Compound: 8f
Cytotoxicity against human UO-31 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
Cytotoxicity against human UO-31 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
[PMID: 36395650]
In Vitro

VEGFR-2-IN-30 (compound 8f) (10 μM) inhibits UO-31 cell growth by 35%[1].
VEGFR-2-IN-30 (10 μg/mL, 72 h) inhibits HUVEC cell migration[1].
VEGFR-2-IN-30 (5.29 μM, 24 h) arrests UO-31 cells at the S phase[1].
VEGFR-2-IN-30 (5.29 μM, 24 h) induces UO-31 cell apoptosis[1].
VEGFR-2-IN-30 (5.29 μM, 24 h) increases the Bax level and down-regulates Bcl-2 level in UO-31 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay [1]

Cell Line: NHUVEC
Concentration: 10 μg/mL
Incubation Time: 72 h
Result: Inhibited cell migration by 58.52%.

Apoptosis Analysis[1]

Cell Line: UO-31 cell
Concentration: 5.29 μM
Incubation Time: 24 h
Result: Increased early apoptotic cells from 0.61% to 23.51% and late apoptotic cells from 0.13% to 9.28%.
Increased the level of active caspase-3.
Molecular Weight

607.10

Formula

C28H23ClN6O4S2

CAS No.
SMILES

O=C(NC1=CC=C(C=C1)S(=O)(NC2=NN=C(C=C2)Cl)=O)CSC3=NC4=CC=CC=C4C(N3CCC5=CC=CC=C5)=O

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
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Product Name:
VEGFR-2-IN-30
Cat. No.:
HY-151969
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