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ATR inhibitor

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製品番号 製品名 Target 研究分野 構造式
  • HY-19323
    Ceralasertib
    55+ Cited Publications

    AZD6738

    ATM/ATR Cancer
    Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.
    Ceralasertib
  • HY-13902
    Berzosertib
    20+ Cited Publications

    VE-822; VX-970; M6620

    ATM/ATR Apoptosis STING Caspase Infection Metabolic Disease Cancer
    Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
    Berzosertib
  • HY-B0097
    Floxuridine
    10+ Cited Publications

    5-Fluorouracil 2'-deoxyriboside

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV Apoptosis Infection Cancer
    Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
    Floxuridine
  • HY-136270
    Gartisertib
    5 Publications Verification

    VX-803; M4344; ATR inhibitor 2

    ATM/ATR Cancer
    Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
    Gartisertib
  • HY-101566
    Elimusertib
    10+ Cited Publications

    BAY 1895344

    ATM/ATR Cancer
    Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity . Elimusertib can be used for the research of solid tumors and lymphomas .
    Elimusertib
  • HY-12016
    KU-55933
    Maximum Cited Publications
    62 Publications Verification

    ATM/ATR Autophagy Cancer
    KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
    KU-55933
  • HY-139609
    Camonsertib
    2 Publications Verification

    RP-3500; ATR inhibitor 4

    ATM/ATR mTOR Cancer
    Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .
    Camonsertib
  • HY-111451
    Tuvusertib
    1 Publications Verification

    M1774; ATR inhibitor 1

    ATM/ATR Cancer
    Tuvusertib (M1774; ATR inhibitor 1) is a selective and orally active ATR inhibitor extracted from patent WO2015187451A1, compound I-l, with a Ki value below 1 μΜ .
    Tuvusertib
  • HY-157941

    ATM/ATR Checkpoint Kinase (Chk) DNA/RNA Synthesis Cancer
    ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC50 of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer .
    ART0380
  • HY-14731
    VE-821
    50+ Cited Publications

    ATM/ATR Cancer
    VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
    VE-821
  • HY-P991272

    PF-05230900

    Interleukin Related Inflammation/Immunology
    ATR-107 (PF-05230900) is a humanized monoclonal antibody inhibitor that targets the interleukin-21 receptor (IL-21R). The Ka value of ATR-107 is 2-4 nM in cynomolgus monkeys, 16 nM in mice, and 71 nM in rats. ATR-107 can be used in research related to systemic lupus erythematosus and air pouch inflammation .
    ATR-107
  • HY-B0255
    Adefovir dipivoxil
    2 Publications Verification

    GS 0840

    HBV Orthopoxvirus HSV DNA/RNA Synthesis ATM/ATR CDK Infection Cancer
    Adefovir dipivoxil is an orally active adenosine analog and Adefovir prodrug. Adefovir dipivoxil inhibits DNA synthesis, activates the ATR signaling pathway, and disrupts the KCTD12-CDK1 interaction. Adefovir dipivoxil has antiviral activity against PRV, HBV, and orthopoxviruses. Adefovir dipivoxil has inhibitory effects on both lamivudine-resistant and wild-type strains. Adefovir dipivoxil has antitumor activity against lung and colon cancer .
    Adefovir dipivoxil
  • HY-171124

    AZD9592

    Antibody-Drug Conjugates (ADCs) EGFR c-Met/HGFR Topoisomerase DNA/RNA Synthesis Cancer
    Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research .
    Tilatamig samrotecan
  • HY-15520
    CGK733
    5+ Cited Publications

    ATM/ATR Cancer
    CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.
    CGK733
  • HY-15557
    AZ20
    5+ Cited Publications

    ATM/ATR Cancer
    AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).
    AZ20
  • HY-N7046

    Silibinin B

    Amyloid-β Apoptosis JNK p38 MAPK Neurological Disease Cancer
    Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity .
    Silybin B
  • HY-150617
    Lartesertib
    1 Publications Verification

    M4076; ATM inhibitor-5

    ATM/ATR STING PD-1/PD-L1 Cardiovascular Disease Inflammation/Immunology Cancer
    Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
    Lartesertib
  • HY-161615

    PROTACs ATM/ATR Apoptosis Inflammation/Immunology Cancer
    PROTAC ATR degrader-2 is a selective ATR PROTAC degrader. PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 values of 22.9 nM and 34.5 nM, respectively. PROTAC ATR degrader-2 has an IC50 of 29.6 nM against ATR, and its IC50 values against ATM and PI3K are both greater than 2000 nM. PROTAC ATR degrader-2 induces apoptosis, DNA damage, and upregulates p53 expression. PROTAC ATR degrader-2 inhibits cancer cell proliferation through the kinase-independent function of ATR protein. PROTAC ATR degrader-2 is applicable to research related to acute myeloid leukemia .
    PROTAC ATR degrader-2
  • HY-15521
    ETP-46464
    2 Publications Verification

    mTOR ATM/ATR Cancer
    ETP-46464 is an effective mTOR and ATR inhibitor with IC50s of 0.6 and 14 nM, respectively.
    ETP-46464
  • HY-101566A
    Elimusertib hydrochloride
    10+ Cited Publications

    BAY 1895344 hydrochloride

    ATM/ATR Cancer
    Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity . Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas .
    Elimusertib hydrochloride
  • HY-159480

    Src ATM/ATR Apoptosis mTOR AMPK Cancer
    AD1058 is an orally active, selective, and BBB-permeable inhibitor of ATR (IC50: 1.6 nM). AD1058 exhibits anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis. AD1058 is suitable for research on advanced malignancies and brain metastases .
    AD1058
  • HY-112198

    ATM/ATR Cancer
    AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer .
    AZ31
  • HY-13816

    CDK ATM/ATR Cancer
    NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner .
    NU6027
  • HY-19323A
    (S)-Ceralasertib
    2 Publications Verification

    (S)-AZD6738

    ATM/ATR Cancer
    (S)-Ceralasertib ((S)-AZD6738) is the S-enantiomer of Ceralasertib (HY-19323). (S)-Ceralasertib is the inhibitor for ataxia telangiectasia mutated and rad3 related (ATR) .
    (S)-Ceralasertib
  • HY-161138

    BCL6 Apoptosis Cancer
    WK369 is a novel BCL6 small molecule inhibitor, which exhibits excellent anti-ovarian cancer bioactivity, induces cell cycle arrest and causes apoptosis. WK369 can directly bind to the BCL6-BTB domain and block the interaction between BCL6 and SMRT, leading to the reactivation of p53, ATR and CDKN1A .
    WK369
  • HY-N6954
    Garcinone C
    2 Publications Verification

    ATM/ATR STAT CDK Hedgehog Inflammation/Immunology Cancer
    Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active .
    Garcinone C
  • HY-145312

    ATM/ATR Cancer
    ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13) .
    ATR-IN-4
  • HY-P10280

    ATM/ATR Cancer
    ATR kinase substrate peptide (ASELPASQPQPFSAKKK) is a peptide substrate for ATR protein kinase and can be used to detect ATR kinase activity .
    ATR kinase substrate peptide
  • HY-B0097R

    5-Fluorouracil 2'-deoxyriboside (Standard)

    Reference Standards Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV Apoptosis Infection Cancer
    Floxuridine (Standard) is the analytical standard of Floxuridine. This product is intended for research and analytical applications. Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
    Floxuridine (Standard)
  • HY-172448

    ATM/ATR Cancer
    YY2201 is a highly potent and selective ATR inhibitor with an IC50 of 8 nM. YY2201 shows >200-fold more selective for ATR than mTOR. YY2201 inhibits tumor progression in broad-spectrum cancer types (such as lung cancer) .
    YY2201
  • HY-101566S

    BAY 1895344-d3

    ATM/ATR Cancer
    Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity .
    Elimusertib-d3
  • HY-171745

    ATM/ATR Cancer
    ATR-IN-32 is an orally active ATR inhibitor. ATR-IN-32 potently inhibits the proliferation of MIA PaCa-2 cells. ATR-IN-32 exerts significant tumor growth inhibition in mice bearing LOVO and HT-29 xenografts. ATR-IN-32 can be used for the study of cancers mediated by ATR protein kinase, such as colorectal cancer, pancreatic cancer .
    ATR-IN-32
  • HY-147190

    ATM/ATR Cancer
    ATR-IN-19 (Compound 15 R-configure) is an ATR inhibitor .
    ATR-IN-19
  • HY-174828

    PARP ATM/ATR Apoptosis Cancer
    ATR/PARP1-IN-1 is a potent ATR and PARP1 dual inhibitor with IC50s of 17.3 nM and 0.38 nM, respectively. ATR/PARP1-IN-1 effectively reduces cell viability, induces apoptosis and DNA damage. ATR/PARP1-IN-1 significantly impairs triple-negative breast cancer (TNBC) colony formation, migration, and invasion. ATR/PARP1-IN-1 suppresses tumor growth effectively in MDA-MB-468 xenografted mice, with no significant body weight change .
    ATR/PARP1-IN-1
  • HY-145450

    ATM/ATR Cancer
    ATR-IN-9 is a potent inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR) extracted from patent WO2020087170A1, compound 59, has an IC50 of 10 nM .
    ATR-IN-9
  • HY-149952

    ATM/ATR Cancer
    ATR-IN-23 (Compound 34) is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. ATR-IN-23 has potent antiproliferative effects on LoVo cells and synthetic lethality on HT-29 cells, and can be used in the study of DNA damage response (DDR)-deficient cancers .
    ATR-IN-23
  • HY-153462

    ATM/ATR Cancer
    ATR-IN-24 (Compound 1) is a ATR inhibitor. ATR-IN-24 has anticancer activity .
    ATR-IN-24
  • HY-147566

    ATM/ATR Cancer
    ATR-IN-14 (compound 1) is a potent ATR kinase inhibitor. ATR-IN-14 inhibits ATR signaling pathways downstream CHKI protein phosphorylation, with inhibition of 98.03% at 25 nM. ATR-IN-14 shows good anticancer activity in LoVo cells, with an IC50 of 64 nM .
    ATR-IN-14
  • HY-153729

    ATM/ATR Cancer
    ATR-IN-29 is a potent and orally active ATR kinase inhibitor with an IC50 value of 1 nM. ATR-IN-29 shows antiproliferative activity .
    ATR-IN-29
  • HY-147569

    ATM/ATR Cancer
    ATR-IN-17 (compound 88) is a potent ATR kinase inhibitor. ATR-IN-17 shows good anticancer activity in LoVo cells, with an IC50 of 1 nM .
    ATR-IN-17
  • HY-147568

    ATM/ATR Cancer
    ATR-IN-16 (compound 46) is a potent ATR kinase inhibitor. ATR-IN-16 shows good anticancer activity in LoVo cells, with an IC50 of 410 nM .
    ATR-IN-16
  • HY-142671

    ATM/ATR Cancer
    ATR-IN-5 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-5 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent CN112047938A, compound D24) .
    ATR-IN-5
  • HY-153393

    ATM/ATR Cancer
    ATR-IN-21 (compound 60) is a potent ATR inhibitor with an IC50 value of <1000 nM .
    ATR-IN-21
  • HY-142672

    ATM/ATR Cancer
    ATR-IN-6 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-6 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021233376A1, compound A22) .
    ATR-IN-6
  • HY-142924

    ATM/ATR Cancer
    ATR-IN-8 is a potent inhibitor of ATR. ATR is a key enzyme in the homologous recombination repair pathway and belongs to the PIKK family. ATR-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021143821A1, compound 3) .
    ATR-IN-8
  • HY-144435

    ATM/ATR Cancer
    ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. ATR kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing replication stress (RS). ATR-IN-11 is a promising lead compound for subsequent agent discovery targeting ATR kinase. ATR-IN-11 has the potential for the research of cancer disease .
    ATR-IN-11
  • HY-147567

    ATM/ATR DNA-PK PI3K Cancer
    ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively .
    ATR-IN-15
  • HY-144214

    ATM/ATR Cancer
    ATR-IN-10 is a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase with an IC50 value of 2.978 μM.
    ATR-IN-10
  • HY-161838

    ATM/ATR Cancer
    ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
    ICT10336
  • HY-123502

    AZD-6738 formate

    ATM/ATR Cancer
    Ceralasertib formate is a potent, selective and orally active ATR inhibitor with an IC50 value of 1 nM. Ceralasertib formate inhibits cell viability and induces DNA damage. Ceralasertib formate induces cell senescence. Ceralasertib formate shows antitumor activity .
    Ceralasertib formate

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