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Results for "

TGI

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-134886
    PD-1-IN-24

    		PD-1/PD-L1 Cancer
    PD-1-IN-24 (compound 1) is an orally active PD-1 inhibitor .
    PD-1-IN-24
  • HY-149433
    BWA-522

    		Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
    BWA-522
  • HY-158138
    TOPOI/PARP-1-IN-1

    		PARP Topoisomerase Apoptosis Cancer
    TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
    TOPOI/PARP-1-IN-1
  • HY-155356
    YN14

    		PROTACs Ras Cancer
    YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
    YN14
  • HY-155681
    SWS1

    		PD-1/PD-L1 Monoamine Oxidase Cancer
    SWS1 is a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM) with anticancer activity. SWS1 can increase the number of tumor-infiltrating lymphocytes and exhibit anti-tumor efficacy in the B16-F10 mouse model (TGI=66.1%) .
    SWS1
  • HY-156085
    LP23

    		PD-1/PD-L1 Cancer
    LP23 is a non-arylmethylamine PD-1/PD-L1 inhibitor (IC50: 16.7 nM) with anti-tumor activity. LP23 restores immune cell function in HepG2/Jurkat T cells and promotes HepG2 cell death. LP23 is active in vivo in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg) .
    LP23
  • HY-123045
    PNU-292137

    		CDK Cancer
    PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
    PNU-292137
  • HY-155226
    FLT3-IN-21

    		FLT3 Apoptosis Cancer
    FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
    FLT3-IN-21
  • HY-163892
    POLRMT-IN-1

    		DNA/RNA Synthesis Cancer
    POLRMT-IN-1 (compound S7) is a POLRMT inhibitor. POLRMT-IN-1 can be used in cancer-related research .
    POLRMT-IN-1
  • HY-115907
    K20

    		Ras ERK Apoptosis Cancer
    K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity .
    K20
  • HY-161629
    TLR8 agonist 7

    		Toll-like Receptor (TLR) Cancer
    TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98% .
    TLR8 agonist 7
  • HY-161630
    TLR8 agonist 8

    		Toll-like Receptor (TLR) Cancer
    TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89% .
    TLR8 agonist 8
  • HY-161631
    TLR8 agonist 9

    		Toll-like Receptor (TLR) Cancer
    TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97% .
    TLR8 agonist 9
  • HY-161641
    Tubulin polymerization-IN-62

    		Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
    Tubulin polymerization-IN-62
  • HY-168081
    PD-1/PD-L1-IN-52

    		PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-52 (Compound III-5) is an orally active PD-1/PD-L1 inhibitor that blocks the interaction between PD-1 and PD-L1, with an IC50 of 109.9 nM. PD-1/PD-L1-IN-52 exhibits antitumor activity in a C57BL/6 mouse xenograft model implanted with human PD-1-expressing MC38 colon cancer cells, with a TGI of 49.6% .
    PD-1/PD-L1-IN-52
  • HY-120758
    SEL24-B489

    		Pim FLT3 Apoptosis Cancer
    SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively .
    SEL24-B489

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