Search Result
Results for "
VEGFR2-IN-2
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-147133
-
|
VEGFR
|
Cancer
|
VEGFR2-IN-2 (compound 6e) is a potent and selective VEGFR2 inhibitor with an IC50 of 19.32 nM. VEGFR2-IN-2 can be used for researching
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- HY-12018
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PTK787 dihydrochloride; ZK-222584 dihydrochloride; CGP-797870 dihydrochloride
|
VEGFR
Apoptosis
|
Cancer
|
Vatalanib dihydrochloride (PTK787 dihydrochloride) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
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-
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- HY-147872
-
|
VEGFR
Microtubule/Tubulin
Apoptosis
|
Cancer
|
VEGFR-2-IN-22 (Compound 25) is a dual VEGFR-2 and β-tubulin polymerization inhibitor with an IC50 of 19.82 nM against VEGFR-2. VEGFR-2-IN-22 induces apoptosis .
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- HY-155758
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VEGFR
Carbonic Anhydrase
|
Cancer
|
hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-2 inhibits VEGFR-2 (IC50=204 nM) and has high binding activity to hCAs, with Kis of 3.6 nM (hCA IX), 16.1 nM (hCA II), 16.7 nM (hCA XII), and 75.3 nM (hCA I), respectively. hCA/VEGFR-2-IN-2 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
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- HY-161995
-
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Apoptosis
Necroptosis
FGFR
VEGFR
PDGFR
|
Cancer
|
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells .
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- HY-168170
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VEGFR
EGFR
|
Cancer
|
EGFR/VEGFR2-IN-2 (compound 4b) is an dual inhibitor VEGFR-2 and EGFR. .
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-
-
- HY-158328A
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-
-
- HY-169431
-
|
VEGFR
Akt
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells .
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- HY-149675
-
|
VEGFR
c-Met/HGFR
|
Cancer
|
VEGFR-2/c-Met-IN-2 (compound 3e) is a VEGFR-2/c-Met inhibitor, with IC50 values of 83 and 48 nM, respectively. VEGFR-2/c-Met-IN-2 exhibits cytotoxic activity against HCT-116 cell line (IC50: 3.403 µM) .
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-
- HY-151459
-
|
VEGFR
Bacterial
Dihydrofolate reductase (DHFR)
Fungal
|
Infection
Cancer
|
VEGFR-2/DHFR-IN-2 (compound 5b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.623 and 9.085 μM, respectively. VEGFR-2/DHFR-IN-2 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 3.59-8.38 μM. VEGFR-2/DHFR-IN-2 can be used for the research of cancer .
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- HY-12572
-
|
Tie
VEGFR
|
Cancer
|
TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively . TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research .
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- HY-10203
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PTK787; ZK-222584; CGP-79787
|
VEGFR
|
Cancer
|
Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
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- HY-12018A
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PTK787 hydrochloride; ZK-222584 hydrochloride; CGP-797870 hydrochloride
|
VEGFR
Apoptosis
|
Others
Cancer
|
Vatalanib (PTK787; ZK-222584; CGP-797870) hydrochloride is an inhibitor of VEGFR2/KDR with an IC50 of 37 nM .
|
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-
- HY-146492
-
|
VEGFR
Raf
Apoptosis
|
Cancer
|
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase .
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- HY-18926
-
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VEGFR
|
Cancer
|
VEGFR2-IN-7 (compound E) is an inhibitor of VEGFR2. VEGFR2-IN-7 can used in study cancers .
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- HY-18185
-
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VEGFR
|
Cancer
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JNJ 17029259 is an orally active and selective VEGF-R2 kinase inhibitor. JNJ 17029259 inhibits VEGF-mediated signal transduction. JNJ 17029259 has anti-angiogenic activity .
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- HY-12686
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FR148083; L783279; LL-Z 1640-2
|
MAP3K
VEGFR
Antibiotic
|
Infection
Inflammation/Immunology
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5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
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- HY-155763
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VEGFR
Carbonic Anhydrase
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Cancer
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hCA/VEGFR-2-IN-4 (compound 15b) is an indolinylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-4 inhibits VEGFR-2 (IC50=0.811 μM) and has high binding activity to hCAs, with Ki of 3.8 nM (hCA XII), 6.2 nM (hCA IX), 19.8 nM (hCA II), and 35.5 nM (hCA I), respectively. hCA/VEGFR-2-IN-4 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
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- HY-112337
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VEGFR
PDGFR
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Cancer
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VEGFR-2-IN-44 (compound 4b) is a selective VEGF-R2 (Flk-1) inhibitor with an IC50 value of 70 nM. VEGFR-2-IN-44 also inhibits PDGF-Rβ with an IC50 of 920 nM .
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- HY-106374
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VEGFR
|
Cancer
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Elpamotide is an epitope peptide derived from VEGFR2. Elpamotide induces cytotoxic T lymphocytes (CTLs) to kill VEGFR2-expressing endothelial cells. Elpamotide has potential immunostimulatory and antineoplastic activities. Elpamotide can be used in the research of cancer, such as pancreatic cancer .
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- HY-146369
-
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PROTACs
VEGFR
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Cancer
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PROTAC VEGFR-2 degrader-2(PROTAC-4), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM) .
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- HY-138813A
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(E/Z)-SU-12662 hydrochloride
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Others
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Cancer
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(E/Z)-N-Desethylsunitinib hydrochloride ((E/Z)-SU-12662 hydrochloride) is a compound with potential anti-tumor activity that inhibits VEGF-R2 and PDGF-Rβ tyrosine kinases. (E/Z)-N-Desethylsunitinib hydrochloride is the main active metabolite of sunitinib and has the ability to competitively inhibit ATP .
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- HY-P1663
-
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VEGFR
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Others
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ATWLPPR Peptide is a biological active peptide. (This peptide is a specific VEGFR2/KDR heptapeptide antagonist, it binds VEGFR2 (KDR/flk), completely inhibiting VEGF binding to KDR and preventing VEGF-induced angiogenesis in-vivo. It specifically inhibits human endothelial cell proliferation in-vitro and totally abolishes VEGF-induced angiogenesis in-vivo.)
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- HY-15334
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VEGFR
|
Cancer
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CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
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- HY-10260
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Vandetanib
Maximum Cited Publications
22 Publications Verification
ZD6474
|
VEGFR
Autophagy
Apoptosis
|
Cancer
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Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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- HY-10260B
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ZD6474 hydrochloride
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VEGFR
Autophagy
Apoptosis
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Cancer
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Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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- HY-10260A
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ZD6474 trifluoroacetate
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VEGFR
Autophagy
Apoptosis
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Cancer
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Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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-
- HY-169296
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VEGFR
CDK
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Cancer
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IMPDH2-IN-4 (compound 2d), a Mycophenolic acid (HY-B0421) analogue, is a selective IMPDH2 inhibitor with a Ki of 1.8 μM. IMPDH2-IN-4 exhibits good cytotoxic activity against osteosarcoma cancer cell lines. IMPDH2-IN-4 possesses a high affinity for VEGFR-2, CDK2, and IMPDH .
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-
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- HY-10260S1
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Isotope-Labeled Compounds
VEGFR
Autophagy
Apoptosis
|
Cancer
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Vandetanib-d4 is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].
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- HY-10260S
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ZD6474-d6
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Isotope-Labeled Compounds
VEGFR
Autophagy
Apoptosis
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Cancer
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Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
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- HY-10260R
-
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VEGFR
Autophagy
Apoptosis
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Cancer
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Vandetanib (Standard) is the analytical standard of Vandetanib. This product is intended for research and analytical applications. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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- HY-10260S2
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ZD6474-13C6
|
Isotope-Labeled Compounds
VEGFR
Autophagy
Apoptosis
|
Cancer
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Vandetanib-13C6 is a deuterated labeled Vandetanib . Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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- HY-168655
-
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Apoptosis
EGFR
VEGFR
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Cancer
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EGFR/VEGFR2-IN-3 (compound 9) is a potent EGFR and VEGFR-2 inhibitor with IC50 values of 0.129, 0.142, 3.428 µM for EGFR, VEGFR-2, COX-2, respectively. EGFR/VEGFR2-IN-3 shows cytotoxicity. EGFR/VEGFR2-IN-3 induces apoptosis and cell cycle arrest at G2/M phase .
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- HY-149630
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VEGFR
HDAC
Apoptosis
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Cancer
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VEGFR2/HDAC1-IN-1 (compound 13) is a potent VEGFR-2/HDAC dual inhibitor, with IC50s of 57.83 nM and 9.82 nM, respectively. VEGFR2/HDAC1-IN-1 arrests the cell cycle at the S and G2 phases, and induces apoptosis in HeLa cells. VEGFR2/HDAC1-IN-1 exhibits anti-angiogenic effect .
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- HY-18187
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Apoptosis
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Cancer
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Ki 23057 is a competitive, orally active inhibitor for tyrosine kinase, which inhibits the phosphorylation of K-samII/FGF-R2, VEGF-R1, VEGF-R2, PDGF-Rβ and c-Kit, with IC50s of 88, 69, 83, 100 and 480 nM. Ki 23057 inhibits the proliferation of sclerogastric cancer cells OCUM-2MD3 and OCUM-8, and induces apoptosis. Ki 23057 exhibits antitumor efficacy in mouse models .
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- HY-112306
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DCC-2618
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c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
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Cancer
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Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
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-
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- HY-146138
-
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EGFR
VEGFR
Casein Kinase
Topoisomerase
Microtubule/Tubulin
Apoptosis
|
Cancer
|
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis .
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- HY-155760
-
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VEGFR
Carbonic Anhydrase
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Cancer
|
hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells .
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-
-
- HY-116116
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SIM010603
|
c-Kit
RET
VEGFR
|
Cancer
|
Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis .
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-
- HY-141685
-
|
CDK
GSK-3
VEGFR
FGFR
|
Cancer
|
3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer .
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-
-
- HY-164529
-
|
Raf
Ras
MEK
ERK
VEGFR
Tie
c-Fms
|
Cancer
|
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
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-
- HY-13590
-
|
VEGFR
|
Cancer
|
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1663
-
|
VEGFR
|
Others
|
ATWLPPR Peptide is a biological active peptide. (This peptide is a specific VEGFR2/KDR heptapeptide antagonist, it binds VEGFR2 (KDR/flk), completely inhibiting VEGF binding to KDR and preventing VEGF-induced angiogenesis in-vivo. It specifically inhibits human endothelial cell proliferation in-vitro and totally abolishes VEGF-induced angiogenesis in-vivo.)
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- HY-P5438
-
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Peptides
|
Others
|
Srctide is a biological active peptide. (This is a peptide substrate for many protein kinases, such as Blk, BTK, cKit, EPHA1, EPHB2, EPHB3, ERBB4, FAK, Flt3, IGF-1R, ITK, Lck, MET, MUSK, Ret, Src, TIE2, TrkB, VEGF-R1 (Flt-1) and VEGF-R2 (KDR).)
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-
- HY-106374
-
|
VEGFR
|
Cancer
|
Elpamotide is an epitope peptide derived from VEGFR2. Elpamotide induces cytotoxic T lymphocytes (CTLs) to kill VEGFR2-expressing endothelial cells. Elpamotide has potential immunostimulatory and antineoplastic activities. Elpamotide can be used in the research of cancer, such as pancreatic cancer .
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- HY-P5527F
-
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Peptides
|
Others
|
FAM-CSKtide is a biological active peptide. (This is a FAM labeled peptide substrate (Abs/Em = 494/521 nm) for C-terminal Src kinase (Csk) and many other kinases such as Axl, cKit, ERBB4, Fes, Flt3, IGF-1 R, MET, MUSK, PYK2, Ret, TIE2, TrkA, VEGF-R1 and VEGF-R2.)
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10260S1
-
|
Vandetanib-d4 is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].
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-
- HY-10260S
-
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Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
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-
- HY-10260S2
-
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Vandetanib-13C6 is a deuterated labeled Vandetanib . Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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