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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
15 Results for "
BRCA mutant cancer
" in MedChemExpress (MCE) Product Catalog:
Products (15)
15 Results for "BRCA mutant cancer" in MCE Product Catalog:
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5 Cited Publications
Synonyms: SHR3162; Fuzuloparib
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
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1 Cited Publications
Cat. No.: HY-170620
PARP1 PROTAC 180055 is a PARP1 PROTAC degrader that recruits VHL, with DC50 values of 180 nM and 240 nM in T47D and MDA-MB-231 cells, respectively. PARP1 PROTAC 180055 selectively kills BRCA-mutant tumor cells by inducing PARP1 ubiquitination and proteasomal degradation, thereby blocking PARylation, NAD + depletion and DNA trapping. PARP1 PROTAC 180055 can be used in the research of breast cancer, ovarian cancer, colorectal cancer, acute T-lymphoblastic leukemia, prostate cancer and osteosarcoma .
Cat. No.: HY-161430
CAS No.: 3035072-49-9
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RTx-161 is a DNA polymerase θ inhibitor with an IC50 of 4.1 nM. RTx-161 induces DNA damage, PARP cleavage, apoptosis, and selectively kills homologous recombination-deficient (HRD) cells. RTx-161 acts synergistically with PARP inhibitors to suppress PARP inhibitor resistance in cancer cells. RTx-161 can be used for the research of BRCA G12C mutant cancer and HR-deficient cancers .
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-179219S
CAS No.: 3035072-99-9
Cat. No.: HY-179582
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PROTAC DNPH1 Degrader 1 is a potent PROTAC DNPH1 degrader with a DC50 of 28 nM. PROTAC DNPH1 Degrader 1 mediates proteasome- and VHL-dependent DNPH1 knockdown, drives DNPH1 ubiquitination and proteasomal degradation. PROTAC DNPH1 Degrader 1 can be used for the research of brca1 mutant cancer .
Cat. No.: HY-153755
CAS No.: 2923356-52-7
Synonyms: Polθ-IN-7
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ART6043 (Polθ-IN-7) is an orally active, selective allosteric DNA polymerase θ (Polθ) inhibitor with an IC50 of 1.3 nM. ART6043 blocks microhomology-mediated end joining (MMEJ) by inhibiting the polymerase function of Polθ. ART6043 suppresses the survival of homologous recombination-deficient (HRD) cells and enhances the antitumor effects of PARP inhibitors. ART6043 can be used in studies of HRD tumors, including BRCA1-mutant triple-negative breast cancer, BRCA2-deficient colorectal cancer, RAD51C-deficient gastric cancer, and others .
Cat. No.: HY-174442
PARP1-IN-40 is a highly selectively and orally active PARP1 inhibitor (IC50: 0.19 nM for PARP1, 26 nM for PARP2). PARP1-IN-40 kills tumor cells by inhibiting PARP1, leading to accumulation of DNA damage. PARP1-IN-40 has high antitumor activity against BRCA mutant MDA-MB-436 cells. PARP1-IN-40 can be used in combination with chemotherapy for cancer-related research .
Cat. No.: HY-189005
PARP1-IN-60 is an orally active PARP1 inhibitor with a human IC50 of 2.4 nM. PARP1-IN-60 selectively inhibits PARP1-mediated poly (ADP-ribosylation) (PARylation) compared with PARP2. PARP1-IN-60 induces DNA damage, G2/M phase arrest and antiproliferative activity in BRCA-deficient cells. PARP1-IN-60 can be used in the research of BRCA-mutant cancers and colorectal cancer .
Cat. No.: HY-P86790
Synonyms: BRCA 2 antibody; BRCA1/BRCA2 containing complex subunit 2 antibody; BRCA2 antibody; BRCA2, DNA repair associated antibody; BRCA2_HUMAN antibody; BRCC 2 antibody; BRCC2 antibody; Breast and ovarian cancer susceptibility gene early onset antibody; breast and ovarian cancer susceptibility protein 2 antibody; Breast cancer 2 early onset antibody; BRCA 2 antibody; BRCA1/BRCA2 containing complex subunit 2 antibody; BRCA2 antibody; BRCA2, DNA repair associated antibody; BRCA2_HUMAN antibody; BRCC 2 antibody; BRCC2 antibody; Breast and ovarian cancer susceptibility gene early onset antibody; breast and ovarian cancer susceptibility protein 2 antibody; Breast cancer 2 early onset antibody; Breast cancer 2 tumor suppressor antibody; Breast cancer susceptibility protein BRCA2 antibody; Breast cancer type 2 susceptibility protein antibody; BROVCA2 antibody; FACD antibody; FAD 1 antibody; FAD antibody; FAD1 antibody; FANCB antibody; FANCD 1 antibody; FANCD antibody; FANCD1 antibody; FANCD1 gene antibody; Fanconi anemia complementation group D1 antibody; Fanconi anemia group D1 protein antibody; GLM3 antibody; mutant BRCA2 antibody; OTTHUMP00000018803 antibody; OTTHUMP00000042401 antibody; PNCA2 antibody; XRCC11 antibody;
Cat. No.: HY-183363
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USP1-IN-17 is an orally active USP1/UAF1 complex inhibitor. USP1-IN-17 exhibits potent anti-proliferative activity against BRCA1-mutant human breast cancer MDA-MB-436 cells, with an IC50 value of 8.1 nM. USP1-IN-17 binds to USP1 to stabilize the enzyme conformation, impairs deubiquitination function, elevates the monoubiquitination level of PCNA, inhibits cancer cell proliferation, and induces DNA damage accumulation. USP1-IN-17 can be used for the research of BRCA1-mutated cancers .
Cat. No.: HY-183765
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PARP1/PKM2-IN-1 is a dual PARP1/PKM2 inhibitor, with an IC50 of 39.5 nM against PARP1, and IC50 values of 261 nM (recombinant PKM2) and 50 nM (dimeric PKM2) against PKM2. PARP1/PKM2-IN-1 reduces the dimerization of PKM2 and decreases its nuclear accumulation level. PARP1/PKM2-IN-1 also selectively downregulates PKM2 mRNA and impairs poly (ADP-ribose)-mediated nuclear retention of PKM2. PARP1/PKM2-IN-1 exhibits antiproliferative activity and inhibits the formation of 3D cancer spheroids. PARP1/PKM2-IN-1 can be used in research related to mammary adenocarcinoma, triple-negative breast cancer, BRCA1-mutant triple-negative breast cancer, and prostate adenocarcinoma .
Cat. No.: HY-185459
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PCIP-1 is a PARP2 inhibitor. PCIP-1 recruits BET proteins to PARP2 to inhibit DNA repair, acts via event-driven pharmacology, and does not inhibit PARP-catalyzed PARylation. PCIP-1 inhibits DNA repair, thereby inducing synthetic lethality in homologous recombination-deficient cancer cells and increasing the sensitivity of PARP1-knockout cells. PCIP-1 can be used in the research of homologous recombination-deficient cancers, T-cell acute lymphoblastic leukemia, and BRCA-mutant cancers .
Cat. No.: HY-181842
PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic 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
