Talazoparib (BMN 673)

目录号:S7048 别名: LT-673

Talazoparib (BMN 673) Chemical Structure

Molecular Weight(MW): 380.35

Talazoparib (BMN 673)是一种新型的PARP抑制剂,无细胞试验中对PARP1的IC50为0.57 nM。它也是有效的PARP-2抑制剂,但不抑制PARG,对PTEN突变型高度敏感。Phase 3。

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客户使用Selleck该产品发表文献12篇:

客户使用该产品的6个实验数据:

  • DNA damage persists on withdrawal of PARPi in RNASEH2AKO cells. Wild-type and RNASEH2AKO HeLa cells were treated with talazoparib and released into fresh medium for the indicated times before being processed for γ-H2AX immunofluorescence and propidium iodide (PI) staining. The γ-H2AX immunofluorescence (pseudocolor plots) and cell cycle (histograms) FACS profiles shown are representative of three biologically independent experiments.

    Nature, 2018, 559(7713):285-289. Talazoparib (BMN 673) purchased from Selleck.

    MDA-MDA-MB-231 and BT549 cells were treated with 10 μM olaparib or 10 nM talazoparib for 24 hours, and subjected to immunoblotting with the indicated antibodies. PD-L1 knockout (K/O) cells were included as a negative control.

    Clin Cancer Res, 2017, 23(14):3711-3720. Talazoparib (BMN 673) purchased from Selleck.

  • Western blot assessment of effects on PAR, PARP, and dsDNA breaks mediated by IMMU-132 plus PARPi in TNBC tumor lines. Cells were plated overnight in 6-well plates before the addition of chemotherapeutics. After a 24-hour incubation, cells were harvested and cell lysates resolved and transferred for Western analysis as described in Materials and Methods. PAR and FL-PARP levels were determined on the same gel. Assessment of dsDNA breaks (p-H2A.X) was calculated as ratios relative to untreated control (Unt) normalized to b-actin protein loading control (Dp-H2A.X). B, HCC1806 cells exposed to rucaparib (Ruc) and IMMU-132 or to (C) talazoparib (Tala) and IMMU-132.

    Clin Cancer Res, 2017, 23(13):3405-3415. Talazoparib (BMN 673) purchased from Selleck.

    PARP inhibition prevents adhesion to and migration of monocytes across BMVEC monolayers preserving the barrier. Primary human monocytes were treated for 24 h with PARPi (AIQ, olaparib, EB47, talazoparib), calcein-labeled, washed, and then added to BMVEC monolayers (untreated or treated for 24 h with TNFα). Treatments were removed prior to the addition of monocytes. Adhesion to (a) and migration of (b) monocytes across blood-brain barrier models were measured and are presented as fold difference compared to TNFα-only control (mean ± SEM) for each treatment from at least quadruplicate determinations, which was assigned a value of 1 (7600 relative fluorescent units for adhesion or equivalent to 37 migrated cells). *P < 0.05, **P < 0.01 indicate significance vs. non-treated. TEER, an indicator of barrier integrity, was continuously measured in BMVEC monolayers treated with or without TNFα following the addition of primary human monocytes that had been treated with PARPi.

    J Neuroinflammation, 2016, 13(1):254.. Talazoparib (BMN 673) purchased from Selleck.

  • BT-549 cells reconstituted with Vet, WT, 336* or PTEN WT HP1aKD were treated with BMN673. Relative cell viability was determined by MTT assay. The results were presented as mean of 3 independent experiments. Error bars indicate s.d.

    Cell Cycle, 2015, 14(14): 2323-32. Talazoparib (BMN 673) purchased from Selleck.

    We treated the FA defective and control lung cancer cell lines H1299D2-down/H1299E and A549D2 down/A549E with BMN673 (0.5 µM). MTT assay was used for the cell viability analysis and an averaged absorbance was recorded 24, 48 and 72 h post treatment.

    Front Oncol, 2014, 4: 368. Talazoparib (BMN 673) purchased from Selleck.

产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述 Talazoparib (BMN 673)是一种新型的PARP抑制剂,无细胞试验中对PARP1的IC50为0.57 nM。它也是有效的PARP-2抑制剂,但不抑制PARG,对PTEN突变型高度敏感。Phase 3。
特性 到目前为止报道的最有效的选择性PARP抑制剂。
靶点
PARP1 [1]
(Cell-free assay)
0.57 nM
体外研究

BMN-673 选择性与PARP 结合,且抑制PARP-介导的通过碱基切除修复途径的单链DNA断裂的修复。增强了DNA链断裂的积累,促进基因组不稳定性,并最终导致细胞凋亡。BMN 673选择性杀死BRCA-1或BRCA-2突变的癌细胞。BMN 673作用于BRCA-1突变 (MX-1,IC50 = 0.3 nM) 和BRCA-2 突变的细胞(Capan-1,IC50 = 5 nM),具有单药细胞毒性。相反, BMN-673 作用于MRC-5正常人类成纤维细胞和其他含野生型BRCA-1 和 BRCA-2基因的肿瘤细胞系,IC50为90 nM到1.9 μM。[1] BMN 673 作用于培养的人类癌细胞,也显著增强Temozolomide 和 SN-38的细胞毒性效果。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BR5FVB1-Akt NFXUfGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnOemwxNjFvMUCwJI5O NITsN|kzPC92OD:3NkBp MoLWbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MUiyOlA1PzZ7Nx?=
BR5FVB1-Akt NUjWW2ZTSXCxcITvd4l{KEG|c3H5 NF3BdI4xNjFvMUCwJI5O NHTIfnM4OiCq MnO5bY5lfWOnczDhdI9xfG:|aYO= M3;OTFI3ODR5Nkm3
Capan-1 NISzWplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF4LkFihKnDueLCiUWuOQKBkcL3TdMg M{HpOFI2QDZ2NUmw
MIA PaCa-2 MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\3WYZKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>? NFTLUXgzPTh4NEW5NC=>
RD MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrrTWM2OD16Lkegcm0> NXPzS3pZOjV{NkO1N|k>
Rh41 M3fMRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LBSGlEPTB;OD6xJI5O NI[0V|MzPTJ4M{WzPS=>
Rh18 MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfBOWlKSzVyPUSuPUBvVQ>? NFn3XFYzPTJ4M{WzPS=>
Rh30 M2K1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTNzLkGgcm0> NUCzR2xYOjV{NkO1N|k>
BT-12 M3vUUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXWTnZpUUN3ME9ihKkyNDByMDDuUS=> MVuyOVI3OzV|OR?=
CHLA-266 M4HWbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLMdoc{UUN3ME9ihKkyNDByMDDuUS=> NUKwWXhHOjV{NkO1N|k>
TC-71 NHPHU4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X1RWlEPTB;Mz63JI5O MXKyOVI3OzV|OR?=
CHLA-9 NHv4W3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfaWo9KSzVyPUiuNkBvVQ>? NWLuc2JPOjV{NkO1N|k>
CHLA-10 M17nd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTZ5Lkigcm0> M2\UdVI2OjZ|NUO5
CHLA-258 NIDZU4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTHTWM2OD12Lk[gcm0> NEjFV28zPTJ4M{WzPS=>
SJ-GBM2 M{joWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnFWJZKSzVyPUG2MlIhdk1? M1\QclI2OjZ|NUO5
NB-1643 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIn6NXFKSzVyPUG4MlQhdk1? NVrXd|B5OjV{NkO1N|k>
NB-EBc1 M2Didmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJ3Lkigcm0> MXmyOVI3OzV|OR?=
CHLA-90 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHuV4tKSzVyPvMAjVEtODByIH7N NEXPVnozPTJ4M{WzPS=>
CHLA-136 MlzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILYNmNKSzVyPUG0MlIhdk1? NFn4fZUzPTJ4M{WzPS=>
NALM-6 M2D5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfDdG1sUUN3ME20PUBvVQ>? NHH3eVMzPTJ4M{WzPS=>
COG-LL-317 NIH4PYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTTTWM2OD17LkSgcm0> NEfnNIUzPTJ4M{WzPS=>
RS4;11 M{LKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jXR2lEPTB;NUKuOkBvVQ>? NY[4OHZbOjV{NkO1N|k>
MOLT-4 NUfCfpVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3oS|dKSzVyPUG2MlYhdk1? M1;6bVI2OjZ|NUO5
CCRF-CEM NGC0cplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTZ7Nz6zJI5O MU[yOVI3OzV|OR?=
Kasumi-1 M3nEbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTd6Nj6yJI5O NHPSW5MzPTJ4M{WzPS=>
Karpas-299 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTd3Lkegcm0> MoP5NlUzPjN3M{m=
Ramos-RA1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTZ6LkOgcm0> NH3qRoIzPTJ4M{WzPS=>
DT40 M3O0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DNZ2lEPTB;NDDuUS=> MWCyOFM2PjhzMx?=
DU145 NUT6ZpY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LFO2lEPTB;MUGgcm0> M2TCc|I1OzV4OEGz
H209 M33BT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\ES3JKSzVyPUGuO{BvVQ>? NG\JW44zPDB5N{O1NC=>
H1048 NHjOWVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjaVXVKSzVyPUKuNkBvVQ>? M36weFI1ODd5M{Ww
H524 NHuzb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3RTWM2OD1|LkGgcm0> MYSyOFA4PzN3MB?=
H1930 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXKTWM2OD12LkGgcm0> NWXSPGhjOjRyN{ezOVA>
H69 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvETWM2OD13LkKgcm0> NVXWd49lOjRyN{ezOVA>
H2081 M{O4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn3XIZKSzVyPU[uN{BvVQ>? MkO3NlQxPzd|NUC=
H2107 MkXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3ETWM2OD15LkOgcm0> M2\n[VI1ODd5M{Ww
H1092 M2rxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjlTWM2OD16Lkmgcm0> NWjUNW9iOjRyN{ezOVA>
DMS-79 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LTbGlEPTB;OT6zJI5O NI\IV4UzPDB5N{O1NC=>
H446 NFvsR|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfnUlVKSzVyPUGzJI5O NYC3O5ozOjRyN{ezOVA>
COR-L279 M1[5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn5dHlbUUN3ME2xOUBvVQ>? NF7Xem0zPDB5N{O1NC=>

... Click to View More Cell Line Experimental Data

体内研究 在大鼠的药代动力学研究中,BMN673每天单独给药,具有>50%口服生物有效性和药代动力学特性。在MX-1移植瘤肿瘤模型研究中, BMN 673每天口服给药,显著增强细胞毒性疗法的抗肿瘤效果,这种作用具有剂量依赖性。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:

[2]

+ 展开
  • Animal Models: MX-1模型(BRCA-1缺陷的)
  • Formulation: --
  • Dosages: 0.33 mg/kg/day,每天一次
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 38 mg/mL warmed (99.9 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 380.35
化学式

 

C19H14F2N6O
 
CAS号 1207456-01-6
稳定性 powder
in solvent
别名 LT-673

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03875313 Recruiting Solid Tumor|Clear Cell Renal Cell Carcinoma|TNBC - Triple-Negative Breast Cancer|Colorectal Cancer|CRC|RCC|ccRCC Calithera Biosciences Inc March 2019 Phase 1|Phase 2
NCT03875313 Recruiting Solid Tumor|Clear Cell Renal Cell Carcinoma|TNBC - Triple-Negative Breast Cancer|Colorectal Cancer|CRC|RCC|ccRCC Calithera Biosciences Inc March 2019 Phase 1|Phase 2
NCT03672773 Recruiting Recurrent Extensive Stage Small Cell Lung Carcinoma|Refractory Extensive Stage Small Cell Lung Carcinoma Jonsson Comprehensive Cancer Center|Translational Research in Oncology|National Cancer Institute (NCI) October 31 2018 Phase 2
NCT03672773 Recruiting Recurrent Extensive Stage Small Cell Lung Carcinoma|Refractory Extensive Stage Small Cell Lung Carcinoma Jonsson Comprehensive Cancer Center|Translational Research in Oncology|National Cancer Institute (NCI) October 31 2018 Phase 2
NCT03637491 Recruiting Pancreatic Cancer|Non-Small Cell Lung Cancer|Cancer Pfizer|Array BioPharma August 15 2018 Phase 2
NCT03499353 Recruiting Early Breast Cancer Pfizer August 27 2018 Phase 2

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    Which solvent do you recommend to dilute the inhibitor for in vivo study in mice?

  • 回答:

    BMN673 (S7048) can be dissolved in vehicle (10% DMAc, 6% Solutol, and 84% PBS) according to the paper: http://clincancerres.aacrjournals.org/content/19/18/5003.full. Quote from Method and Material section "Xenograft experiments: BMN 673 (various doses as indicated), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) was administered by oral gavage"

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID