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DLD-1 xenografts

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-177512
    MSC778

    		FLAP Cancer
    MSC778 is an effective and orally active flap endonuclease 1 (FEN1) inhibitor with an IC50 of 3 nM and a KD of 2.9 nM. MSC778 exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively kills BRCA2-deficient cells and potentiates the activity of Niraparib (HY-10619) to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft. MSC778 can be used in the research of colorectal cancer .
    MSC778
  • HY-158346
    RP-2119

    		DNA/RNA Synthesis Cancer
    RP-2119 is an orally bioactive Polymerase Theta (Polθ) inhibitor, with an IC50 of 0.7 nM against human Polθ ATPase. RP-2119 reduces Polθ activity and exerts antiproliferative effects in BRCA2-deficient cancer cells. RP-2119 exhibits antitumor activity in BRCA2-deficient cancer cell xenograft mouse models . RP-2119 can be used for the research of cancer and homologous recombination-deficient cancers, including brca1/brca2-mutant cancers and shld2-mutant cancers .
    RP-2119
  • HY-165606
    SB-T-1214

    		Oct3/4 c-Myc Apoptosis Cancer
    SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133 +/CD44 + cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers .
    SB-T-1214
  • HY-16491
    Tesetaxel

    DJ-927

    		 Microtubule/Tubulin Cancer
    Tesetaxel (DJ-927) is an orally active and brain-penetrant taxane tubulin inhibitor. Tesetaxel inhibits tubulin depolymerization with an IC50 of 0.44 μM. Tesetaxel inhibits cancer cells proliferation and shows potent antitumor activity against P-glycoprotein-positive cancer cells. Tesetaxel can be used for the research of cancer, such as solid tumors, liver metastasis, and advanced breast cancer .
    Tesetaxel
  • HY-179413
    Polθ-IN-9

    		DNA/RNA Synthesis Cancer
    Polθ-IN-9 is an orally active Polθ polymerase inhibitor (IC50 = 9.6 nM, Kd = 47.5 nM). Polθ-IN-9 shows remarkable selectivity with no inhibitory activity against other human DNA polymerases, including Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. Polθ-IN-9 exhibits strong antiproliferative activity in DLD1 BRCA2 KO cells (IC50 = 2.9 μM), and high sensitivity to MDA-MB-436 cells (IC50 = 4.9 μM). Polθ-IN-9 increases DNA damage accumulation, induces γH2AX levels, and inhibits tumor growth in combination with Olaparib (HY-10162), in the MDA-MB-436 xenograft model. Polθ-IN-9 can be used for the research of homologous recombination (HR)-deficient cancers such as breast cancer .
    Polθ-IN-9
  • HY-183630
    AZD4956

    		DNA/RNA Synthesis Cancer
    AZD4956 is a potent and selective DNA polymerase theta (POLQ) inhibitor. AZD4956 exhibits an IC50 value of less than 3 μmol/L against POLQ and 3.4 μmol/L against MMEJ. AZD4956 suppresses the MMEJ pathway and enhances the activity of DNA-damaging agents in HRR-deficient cellular contexts. AZD4956 shows antitumor activity in BRCA1/2-mutated triple-negative breast cancer and prostate cancer models. AZD4956 can be used for the study of homologous recombination-deficient tumors .
    AZD4956

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