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VEGFR-2 selectivity

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45

Inhibitors & Agonists

1

Natural
Products

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-147133
    VEGFR2-IN-2

    		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
    VEGFR2-IN-2
  • HY-145849
    VEGFR2-IN-1

    		VEGFR Cancer
    VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition .
    VEGFR2-IN-1
  • HY-149361
    VEGFR2-IN-4

    		VEGFR Inflammation/Immunology
    VEGFR2-IN-4 (compound 25) is a potent and selective VEGFR2 kinase inhibitor, with a GI50 of 0.7 nM. VEGFR2-IN-4 shows anti-angiogenic effect. VEGFR2-IN-4 can be used for the research of rheumatoid arthritis .
    VEGFR2-IN-4
  • HY-146539
    HDAC-IN-35

    		HDAC VEGFR Cancer
    HDAC-IN-35 (Compound 14) is a potent, selective HDAC and VEGFR-2 inhibitor, with IC50 values of 0.166 and 13.2 µM for HDAC6 and VEGFR-2, respectively .
    HDAC-IN-35
  • HY-112337
    VEGFR-2-IN-44

    		VEGFR PDGFR Cancer
    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 .
    VEGFR-2-IN-44
  • HY-149024
    VEGFR-2-IN-23

    		VEGFR Apoptosis MDM-2/p53 Cancer
    VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cell cycle arrest at G1 phase .
    VEGFR-2-IN-23
  • HY-15467
    ZM323881

    		VEGFR Cancer
    ZM323881 is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
    ZM323881
  • HY-15467A
    ZM323881 hydrochloride
    2 Publications Verification

    		 VEGFR Cancer
    ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
    ZM323881 hydrochloride
  • HY-108443
    DMH4

    		VEGFR Cancer
    DMH4 is a potent and selective inhibitor of VEGFR2 with an IC50 of 0.16 µM .
    DMH4
  • HY-13302
    CP-547632

    		VEGFR FGFR Cancer
    CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy .
    CP-547632
  • HY-13302B
    CP-547632 hydrochloride

    		VEGFR FGFR Cancer
    CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy .
    CP-547632 hydrochloride
  • HY-100394
    NVP-BAW2881

    BAW2881

    		 Tie VEGFR Endocrinology Cancer
    NVP-BAW2881 (BAW2881) is a potent and selective VEGFR2 inhibitor with an IC50 of 4 nM.
    NVP-BAW2881
  • HY-13302C
    CP-547632 TFA

    		VEGFR FGFR Cancer
    CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy .
    CP-547632 TFA
  • HY-19326
    SU1498
    5 Publications Verification

    AG 1498; Tyrphostin SU 1498

    		 VEGFR Inflammation/Immunology Cancer
    SU1498 (AG 1498) is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC50 of value of 700 nM .
    SU1498
  • HY-18317
    JNJ-38158471

    		VEGFR RET c-Kit Cancer
    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively .
    JNJ-38158471
  • HY-10799
    EG00229
    5+ Cited Publications

    		 Complement System Cancer
    EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2 .
    EG00229
  • HY-144075
    JAK-IN-19

    		JAK Inflammation/Immunology
    JAK-IN-19 is a potent JAK inhibitor (PBMC IFNγ pIC50=7.2 and HLF Eotaxin pIC50=7.7). JAK-IN-19 has good retentive properties in the lung via mitigating being metabolized by Aldehyde Oxidase (AO), with diminished VEGFR2 selectivity (VEGFR2 pIC50=7.0, Aurora B pIC50=5.8) .
    JAK-IN-19
  • HY-155684
    SA-PA

    		PROTACs VEGFR PDGFR Ephrin Receptor Cancer
    SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues .
    SA-PA
  • HY-10321
    PD173074
    Maximum Cited Publications
    10 Publications Verification

    		 FGFR VEGFR Apoptosis Cancer
    PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.
    PD173074
  • HY-18185
    JNJ 17029259

    		VEGFR Cancer
    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 .
    JNJ 17029259
  • HY-120640
    BMS-605541

    		VEGFR PDGFR Cancer
    BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research .
    BMS-605541
  • HY-13342AS
    Apatinib-d8 free base

    YN968D1-d8 free base

    		 Src VEGFR Autophagy c-Kit RET Cancer
    Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
    Apatinib-d8 free base
  • HY-119757
    Tyrphostin AG1433

    SU1433; AG1433

    		 PDGFR VEGFR Cancer
    Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation .
    Tyrphostin AG1433
  • HY-155685
    SA-VA

    		PROTACs VEGFR Ephrin Receptor Apoptosis Cancer
    SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase .
    SA-VA
  • HY-12076
    BMS 777607
    Maximum Cited Publications
    10 Publications Verification

    BMS 817378

    		 c-Met/HGFR TAM Receptor Cancer
    BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases .
    BMS 777607
  • HY-12686
    5Z-7-Oxozeaenol
    Maximum Cited Publications
    10 Publications Verification

    FR148083; L783279; LL-Z 1640-2

    		 MAP3K VEGFR Antibiotic Infection Inflammation/Immunology
    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.
    5Z-7-Oxozeaenol
  • HY-135366
    HPN-01

    		IKK Inflammation/Immunology
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .
    HPN-01
  • HY-15391
    Lucitanib
    5+ Cited Publications

    E-3810

    		 VEGFR FGFR Cancer
    Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
    Lucitanib
  • HY-147714
    FGFR3-IN-2

    		FGFR VEGFR Cancer
    FGFR3-IN-2 (compound 18b) is a potent and selective FGFR3 inhibitor, with IC50s of 4.1 nM and 570 nM for FGFR3 and VEGFR2, respectively. FGFR3-IN-2 can be used for the research of bladder cancer .
    FGFR3-IN-2
  • HY-10542
    GW 5074
    5+ Cited Publications

    		 Raf Apoptosis Cancer
    GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms .
    GW 5074
  • HY-149099
    RET-IN-22

    		RET Cancer
    RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
    RET-IN-22
  • HY-112306
    Ripretinib

    DCC-2618

    		 c-Kit PDGFR FLT3 VEGFR Apoptosis Cancer
    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 .
    Ripretinib
  • HY-139590
    Zeteletinib

    BOS-172738; DS-5010

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
    Zeteletinib
  • HY-108444
    (Z)-FeCP-oxindole

    		VEGFR Cancer
    (Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM .
    (Z)-FeCP-oxindole
  • HY-108444A
    (E)-FeCP-oxindole

    		VEGFR Cancer
    (Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM .
    (E)-FeCP-oxindole
  • HY-139590A
    Zeteletinib hemiadipate

    BOS-172738 hemiadipate; DS-5010 hemiadipate

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
    Zeteletinib hemiadipate
  • HY-10032
    PF 477736
    5 Publications Verification

    PF 00477736

    		 Checkpoint Kinase (Chk) VEGFR Src c-Fms Aurora Kinase FGFR FLT3 RET CDK Cancer
    PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
    PF 477736
  • HY-112780
    UC2288
    2 Publications Verification

    		 MDM-2/p53 Cancer
    UC2288 is a novel, cell-permeable, and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM .
    UC2288
  • HY-12010
    BMS-599626 Hydrochloride
    3 Publications Verification

    AC480 Hydrochloride

    		 EGFR Cancer
    BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
    BMS-599626 Hydrochloride
  • HY-10408
    Ki20227
    5 Publications Verification

    		 c-Fms VEGFR c-Kit PDGFR Inflammation/Immunology
    Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction .
    Ki20227
  • HY-116624
    MAZ51
    2 Publications Verification

    		 VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity .
    MAZ51
  • HY-10251
    BMS-599626

    AC480

    		 EGFR Cancer
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
    BMS-599626
  • HY-112809
    GSK2646264

    		Syk Src LRRK2 GSK-3 JAK VEGFR Aurora Kinase Inflammation/Immunology
    GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin .
    GSK2646264
  • HY-141685
    3-Methylthienyl-carbonyl-JNJ-7706621

    		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 .
    3-Methylthienyl-carbonyl-JNJ-7706621
  • HY-147695
    c-Met-IN-12

    		c-Met/HGFR Cancer
    c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy .
    c-Met-IN-12

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