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  4. Berzosertib hydrochloride

Berzosertib hydrochloride  (Synonyms: VE-822 hydrochloride; VX-970 hydrochloride; M6620 hydrochloride)

目录号: HY-13902A
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Berzosertib (VE-822) hydrochloride 是一种具有口服活性、可穿透血脑屏障的、选择性 ATR 激酶抑制剂。Berzosertib hydrochloride 可阻断 ATR 激酶活性，消除 G2/M 细胞周期检查点，损伤 DNA 损伤修复功能。Berzosertib hydrochloride 可诱导细胞凋亡 (apoptosis)，抑制克隆迁移与细胞增殖，并激活癌细胞中的 cGAS-STING 轴。Berzosertib hydrochloride 可用于癌症相关研究，如头颈部鳞状细胞癌、结直肠癌等。

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CAS No. : 1428935-04-9

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Berzosertib hydrochloride 相关抗体

Top Publications Citing Use of Products

    Berzosertib hydrochloride purchased from MCE. Usage Cited in: Cancer Commun (Lond). 2023 Apr;43(4):435-454.  [Abstract]

    Berzosertib (60 mg/kg) was administered by gavage 2 h before IR and consecutively for the next three days. Representative IHC images of CD3 staining of MC38 tumors were shown.

    Berzosertib hydrochloride purchased from MCE. Usage Cited in: Cancer Commun (Lond). 2023 Apr;43(4):435-454.  [Abstract]

    Berzosertib (60 mg/kg) was administered by gavage 2 h before IR and consecutively for the next three days. Representative flow cytometry images and quantitative analysis of TILs in CT26 tumors were obtained.

    Berzosertib hydrochloride purchased from MCE. Usage Cited in: Cancer Commun (Lond). 2023 Apr;43(4):435-454.  [Abstract]

    Berzosertib (0–2 μM; 24 h). Cell viability assay of multiple CRC cell lines treated with ATRi and IR + ATRi was performed.

    Berzosertib hydrochloride purchased from MCE. Usage Cited in: Cancer Commun (Lond). 2023 Apr;43(4):435-454.  [Abstract]

    Berzosertib (1 μM). Cell cycle distribution analysis of HCT116 and CT26 cells treated with IR and IR + ATRi. Representative flow cytometry images of phospho-histone H3+ cells in HCT116 and CT26 cells were shown.

    Berzosertib hydrochloride purchased from MCE. Usage Cited in: Cancer Commun (Lond). 2023 Apr;43(4):435-454.  [Abstract]

    Berzosertib (1 μM; 14 h). IF images of dsDNA and cGAS staining in HCT116 cells were shown.

    Berzosertib hydrochloride purchased from MCE. Usage Cited in: Cancer Commun (Lond). 2023 Apr;43(4):435-454.  [Abstract]

    Berzosertib (1 μM; 14 h) was used. Immunoblotting of the key proteins from the canonical cGAS-STING axis in multiple CRC cell lines was performed.

    Berzosertib hydrochloride purchased from MCE. Usage Cited in: Eur J Med Chem. 2017 Feb 15:127:691-702.  [Abstract]

    Relative cell viability (%) in MDCK CAIX- and CAIX+ cells exposed to ATR inhibitors (VE-821 and VE-822) or the CAIXi conjugated derivatives in combination with radiation during normoxia (21% O2) and anoxia (≤0.02% O2). Normoxic cells are irradiated with 2 Gy and anoxic cells with 4 Gy to induce similar effects on cell viability.

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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer[1][2][3][4][5][6].

    IC50 & Target[1]

    Caspase-3

     

    ATR

    0.2 nM (Ki)

    ATM

    34 nM (Ki)

    体外研究
    (In Vitro)

    Berzosertib (0.031-1 µM; 72 h) hydrochloride 可降低 Cal-27 和 FaDu 头颈部鳞状细胞癌 (HNSCC) 细胞系的细胞活力，其 IC50 值分别为 0.285 µM 和 0.252 µM[1]。
    Berzosertib (0.125-0.5 µM; 24-48 h) hydrochloride 可抑制 Cal-27 和 FaDu 头颈部鳞状细胞癌 (HNSCC) 细胞的迁移[1]。
    Berzosertib (0.25-0.5 µM; 48 h) hydrochloride 可诱导 Cal-27 和 FaDu 细胞发生凋亡[1]。
    Berzosertib (48-72 h) hydrochloride 可抑制 A549、NCI-H226 和 NCI-H520 细胞的增殖，其 IC50 值处于 1-4 μM 范围[2]。
    Berzosertib (40-80 nM; 1 h) hydrochloride 可增强 A549、NCI-H226 和 NCI-H520 非小细胞肺癌 (NSCLC) 细胞系的放射敏感性[2]。
    Berzosertib (40 nM; 1 h) hydrochloride 可抑制 A549、NCI-H226 和 NCI-H520 非小细胞肺癌 (NSCLC) 细胞系中辐射诱导的 ATR (Thr1989) 磷酸化，且不影响 ATM (Ser1981) 的激活[2]。
    Berzosertib (40 nM; 1 h) hydrochloride 可消除 A549 非小细胞肺癌细胞中辐射诱导的 G2/M 细胞周期检查点，使细胞进入 G1 期[2]。
    Berzosertib (40-80 nM; 1 h) hydrochloride 与 10 Gy 而非 2 Gy 的辐照联合使用时，可增强 A549 非小细胞肺癌细胞中辐射诱导的细胞凋亡[2]。
    Berzosertib (40 nM; 1 h) hydrochloride 可抑制 A549 细胞中的 DNA 双链断裂修复[2]。
    Berzosertib (1 µM; 2 h) hydrochloride 可破坏 HCT116 和 CT26 细胞中辐射诱导的 G2/M 检查点的启动与维持，促进 DNA 损伤后的有丝分裂进入[4]。
    Berzosertib (1 µM; 2 h) hydrochloride 联合 5 Gy 辐照可提高 HCT116 和 CT26 结直肠癌细胞系中的微核形成水平与胞质双链 DNA 含量[4]。
    Berzosertib (1 µM; 2 h) hydrochloride 联合 5 Gy 照射可强效激活经典 cGAS-STING-pTBK1/pIRF3 通路，并在 HCT116、SW480、CT26 和 MC38 细胞中上调干扰素刺激基因 CXCL10、CCL5 和 IFNB 的表达[4]。
    Berzosertib (1 µM; 2 h) hydrochloride 联合 5 Gy 辐照可抑制 SHP1 向 HCT116 细胞中 TRAF6/STING 复合物的募集，增强 TRAF6 与 STING 的相互作用[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Berzosertib hydrochloride 相关抗体:

    Cell Viability Assay[1]

    Cell Line: Cal-27, FaDu cells
    Concentration: 0.031; 0.063; 0.125; 0.25; 0.5; 1 µM
    Incubation Time: 72 h
    Result: Caused a dose-dependent decrease in cell viability in both cell lines.
    Exhibited an IC50 value of 0.285 µM for Cal-27 cells.
    Exhibited an IC50 value of 0.252 µM for FaDu cells.

    Cell Proliferation Assay[1]

    Cell Line: Cal-27, FaDu cells
    Concentration: 0.125; 0.25; 0.5 µM
    Incubation Time: 24 h (Cal-27); 48 h (FaDu)
    Result: Reduced Cal-27 cell gap closure to 82% at 0.25 µM and 50% at 0.5 µM at 24 h, compared to 98% in untreated cells.
    Reduced FaDu cell gap closure to 24% at 0.25 µM and 0.5 µM at 24 h, compared to 41% in untreated cells.
    Significantly inhibited FaDu cell gap closure at 0.5 µM at 48 h.

    Apoptosis Analysis[1]

    Cell Line: Cal-27, FaDu cells
    Concentration: 0.25 µM (Cal-27); 0.5 µM (FaDu)
    Incubation Time: 48 h
    Result: Increased apoptosis levels to 279% of control in Cal-27 cells.
    Increased apoptosis levels to 244% of control in FaDu cells.

    Western Blot Analysis[2]

    Cell Line: A549, NCI-H226, and NCI-H520 cells
    Concentration: 40 nM
    Incubation Time: 1 h
    Result: Did not affect radiation-induced ATM (Ser1981) phosphorylation.
    Diminished radiation-induced activation of p-ATR (Thr1989) in all three cell lines even at 24 h post-radiation.

    Apoptosis Analysis[2]

    Cell Line: A549 cells
    Concentration: 40; 80 nM
    Incubation Time: 1 h
    Result: Showed no increase in apoptosis when combined with 2 Gy radiation.
    Caused a significant increase in apoptosis when combined with 10 Gy radiation, compared to radiation alone.

    Immunofluorescence[2]

    Cell Line: A549 cells
    Concentration: 40 nM
    Incubation Time: 1 h
    Result: Combined with irradiation resulted in a statistically significant increase in the number of γH2AX foci at 8 h and 24 h compared with cells treated with irradiation alone.

    Real Time qPCR[4]

    Cell Line: HCT116, SW480, CT26, MC38
    Concentration: 1 µM
    Incubation Time: 2 h
    Result: Caused a sharp, time-dependent increase in mRNA levels of CXCL10, CCL5, and IFNB in HCT116 and CT26 cells, with peak expression at 8-12 hours post-irradiation.
    Induced significant increases in CXCL10, CCL5, and IFNB gene expressions in SW480 and MC38 cells compared to irradiation alone.
    体内研究
    (In Vivo)

    Berzosertib (60 mg/kg；口服；每日一次；连续 10 天；2 Gy 局部肿瘤照射前 1 小时) hydrochloride 与每日 2 Gy 局部照射协同作用，可延缓小鼠皮下非小细胞肺癌脑转移 PDX 模型的肿瘤生长[2]。
    Berzosertib (60 mg/kg；口服；每日 1 次；连续 5 天；于 2.5 Gy 全脑照射前 1 小时给药) hydrochloride 联合每日 2.5 Gy 全脑照射，可显著提升小鼠 NSCLC 脑转移异种移植模型的中位总生存期并抑制颅内肿瘤生长[2]。
    Berzosertib (灌胃给药，剂量 60 mg/kg；于 Gy 射线照射前 2 小时给药，随后每日给药 1 次，连续 3 天) hydrochloride 与 5 Gy 照射及抗 PD-L1 联合使用时，在小鼠 MC38 和 CT26 模型中产生抗肿瘤活性[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female Hsd:athymic Nude-Foxn1 mice (6-8-week-old) subcutaneously implantated with UW-lung-16 and UW-lung-18[2]
    Dosage: 60 mg/kg
    Administration: p.o.; daily; 10 days; 1 h before 2 Gy local tumor irradiation
    Result: Delayed growth of UW-lung-16 and UW-lung-18 tumors.
    Reduced estimated tumor growth curve slope for UW-lung-16 tumors significantly lower than alone, with a synergistic effect and dose enhancement factor (DEF) of 1.8.
    Reduced estimated tumor growth curve slope for UW-lung-18 tumors significantly lower than alone, with a synergistic effect and DEF of 1.4.
    Inhibited phospho-Chk1 (Ser345) alone and combined with irradiation.
    Increased cleaved caspase-3 in the combination group.
    Induced significantly more γH2AX foci in the combination group compared to other groups.
    Animal Model: Athymic nude mice intracranial implantation of luciferase-transfected UW-Lung-16 cells[2]
    Dosage: 60 mg/kg
    Administration: p.o.; daily; 5 days; 1 h before 2.5 Gy whole brain irradiation
    Result: Reduced bioluminescence total flux significantly by days 32 and 40 post-implant compared to radiation alone.
    Improved median overall survival to 95 days, compared to 67 days in the radiation alone group.
    Showed no significant difference in body weight between groups during or 40 days post-treatment.
    Animal Model: C57/B6J mice (female, 5-6 weeks old) subcutaneously injected with MC38 cells[4]
    Dosage: 60 mg/kg
    Administration: i.g.; 2 h before Gy IR, then daily for 3 days
    Result: Delayed tumor growth more effectively than dual or monotherapy regimens.
    Led to complete tumor regression in some mice.
    Extended mouse survival compared to other treatment groups.
    Reduced tumor burden (as measured by bioluminescence total flux).
    Decreased Ki67-positive proliferating cells.
    Increased TUNEL-positive apoptotic cells.
    Increased CD3+ and CD8+ tumor-infiltrating lymphocyte counts.
    Elevated levels of CD11c+ MHC-II+ dendritic cells and CD11c+ CD8+ tumor-infiltrating dendritic cells.
    Increased CD86 maturation marker mean fluorescence intensity.
    Activated the canonical cGAS-STING-pTBK1/pIRF3 axis.
    Activated the non-canonical STING-p65 axis.
    Upregulated mRNA expression of innate immune-related genes Cxcl10, Ccl5, and Ifnb.
    Animal Model: Balb/C mice (female, 5-6 weeks old) subcutaneously injected with CT26 cells[4]
    Dosage: 60 mg/kg
    Administration: i.g.; 2 h before Gy IR, then daily for 3 days
    Result: Delayed tumor growth more effectively than dual or monotherapy regimens.
    Extended mouse survival compared to other treatment groups.
    Increased CD3+ and CD8+ tumor-infiltrating lymphocyte counts.
    Elevated levels of CD11c+ MHC-II+ dendritic cells and CD11c+ CD8+ tumor-infiltrating dendritic cells.
    Increased CD86 maturation marker mean fluorescence intensity.
    Activated the canonical cGAS-STING-pTBK1/pIRF3 axis.
    Activated the non-canonical STING-p65 axis.
    Upregulated mRNA expression of innate immune-related genes Cxcl10, Ccl5, and Ifnb.
    Decreased SHP1 mRNA levels and SHP1 interaction with TRAF6/STING via promoting SHP1 SUMOylation at lysine 127.
    分子量

    500.01

    Formula

    C24H26ClN5O3S
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
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    参考文献

    Berzosertib hydrochloride 相关分类

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    Keywords:

    Berzosertib1428935-04-9VE-822VX-970M6620VE822VE 822VX970VX 970M 6620M-6620ATM/ATRApoptosisSTINGCaspaseAtaxia telangiectasia mutatedATM and RAD3 relatedStimulator of Interferon GenesTMEM173MITAERISMPYScolorectal cancernon-small cell lung cancer brain metastaseshead and neck squamous cell carcinomadiffuse midline glioma H3K27-alteredCal-27A549FaDuATR kinasepancreatic ductal adenocarcinomaSHP1Inhibitorinhibitorinhibit

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