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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
3 Results for "
HR-deficient models
" in MedChemExpress (MCE) Product Catalog:
Products (3)
3 Results for "HR-deficient models" in MCE Product Catalog:
Cat. No.: HY-158346
CAS No.: 2922287-81-6
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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 .
Cat. No.: HY-183748
CAS No.: 3082173-75-6
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Polθ-IN-11 is an orally active DNA polymerase θ (Polθ) ATPase inhibitor with an IC50 of 4.3 nM against human targets. Polθ-IN-11 activates the cGAS-STING pathway. Polθ-IN-11 upregulates the expression of PD-L1 in HR-deficient cancer cells. Polθ-IN-11 acts synergistically with PARP inhibition in HR-deficient cancer cells and in vivo xenograft models. Polθ-IN-11 can be used in studies related to HR-deficient cancers .
Cat. No.: HY-179413
CAS No.: 3050552-13-8
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
