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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RMB 3831.14 现货
RMB 7944.13 现货
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客户使用该产品的4个实验数据:

  • 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 M{\pdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HOOVAvOS1zMECgcm0> MV[yOE81QC95MjDo Mn2wbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MoXKNlYxPDd4OUe=
BR5FVB1-Akt MUTBdI9xfG:|aYOgRZN{[Xl? NY\4b5VkOC5zLUGwNEBvVQ>? M17oVVczKGh? MmnnbY5lfWOnczDhdI9xfG:|aYO= MUCyOlA1PzZ7Nx?=
Capan-1 NVTzWZFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LNd2lEPTB;MU[uNQKBkcLz4pEJOU416oDLwsXNxsA> MnKzNlU5PjR3OUC=
MIA PaCa-2 NIPoT5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG3VmRKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>? MYiyOVg3PDV7MB?=
RD MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{H2O2lEPTB;OD63JI5O MkjVNlUzPjN3M{m=
Rh41 NXexWY51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRThwMTDuUS=> M4TjSVI2OjZ|NUO5
Rh18 M4fTVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDUeoZKSzVyPUSuPUBvVQ>? NWfrblIzOjV{NkO1N|k>
Rh30 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTNzLkGgcm0> NIDL[IIzPTJ4M{WzPS=>
BT-12 M3vwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\DO2lEPTB-4pEJNUwxODBibl2= M4fsSVI2OjZ|NUO5
CHLA-266 NEXM[XVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojZTWM2OD8kgJmxMFAxOCCwTR?= NH7MVXQzPTJ4M{WzPS=>
TC-71 Mn\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXlS|NKSzVyPUOuO{BvVQ>? MUmyOVI3OzV|OR?=
CHLA-9 NGXOW4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnLOnQxUUN3ME24MlIhdk1? Ml7hNlUzPjN3M{m=
CHLA-10 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHVT3lKSzVyPU[3Mlghdk1? MYmyOVI3OzV|OR?=
CHLA-258 NXmxS5FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorJTWM2OD12Lk[gcm0> MnixNlUzPjN3M{m=
SJ-GBM2 NUnXOFVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmS1TWM2OD1zNj6yJI5O MV6yOVI3OzV|OR?=
NB-1643 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTF6LkSgcm0> NWjzcY5GOjV{NkO1N|k>
NB-EBc1 M4PTUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfGSVVKSzVyPUK1Mlghdk1? M{HXUFI2OjZ|NUO5
CHLA-90 M1vxOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPtTWM2OD8kgJmxMFAxOCCwTR?= NFHFWY4zPTJ4M{WzPS=>
CHLA-136 NGTrSHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWe5TmtmUUN3ME2xOE4zKG6P M1XJPFI2OjZ|NUO5
NALM-6 M1\reGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHuTWM2OD12OTDuUS=> NFWzZWQzPTJ4M{WzPS=>
COG-LL-317 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3lPFZyUUN3ME25MlQhdk1? MV:yOVI3OzV|OR?=
RS4;11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHviS|RKSzVyPUWyMlYhdk1? MnrFNlUzPjN3M{m=
MOLT-4 MnPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\Yd5BKSzVyPUG2MlYhdk1? M1izOVI2OjZ|NUO5
CCRF-CEM MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzH[5VKSzVyPU[5O{4{KG6P NYPU[HQ4OjV{NkO1N|k>
Kasumi-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17vU2lEPTB;N{i2MlIhdk1? NX60T5FPOjV{NkO1N|k>
Karpas-299 NXyyW4xJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;aTWM2OD15NT63JI5O MYeyOVI3OzV|OR?=
Ramos-RA1 NX7X[npjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPOZo1pUUN3ME22PE4{KG6P Ml\iNlUzPjN3M{m=
DT40 MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDDTWM2OD12IH7N MYeyOFM2PjhzMx?=
DU145 M{jsT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFzIH7N MmnINlQ{PTZ6MUO=
H209 NEHITpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3LTWM2OD1zLkegcm0> M2nXPVI1ODd5M{Ww
H1048 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jxZWlEPTB;Mj6yJI5O MViyOFA4PzN3MB?=
H524 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTNwMTDuUS=> MXqyOFA4PzN3MB?=
H1930 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jyd2lEPTB;ND6xJI5O MUOyOFA4PzN3MB?=
H69 MkD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGi4cnVKSzVyPUWuNkBvVQ>? M4THfVI1ODd5M{Ww
H2081 M{[5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTZwMzDuUS=> NFTnZnkzPDB5N{O1NC=>
H2107 NXrifXY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTdwMzDuUS=> MmjXNlQxPzd|NUC=
H1092 NFT4VoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPteGpKSzVyPUiuPUBvVQ>? NFy5WHYzPDB5N{O1NC=>
DMS-79 NEfCVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nZc2lEPTB;OT6zJI5O MoPENlQxPzd|NUC=
H446 NX\KNIxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF|IH7N NXrWWY45OjRyN{ezOVA>
COR-L279 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorDTWM2OD1zNTDuUS=> MWGyOFA4PzN3MB?=

... 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
NCT03426254 Enrolling by invitation Advanced or Recurrent Solid Tumors|Breast Neoplasm Center Trials & Treatment|BioGene Pharmaceutical February 8 2018 Phase 1
NCT02997163 Recruiting Advanced Solid Tumors Pfizer|Medivation Inc. February 8 2017 Phase 1
NCT02921919 Recruiting Cancer Pfizer|Medivation Inc. November 8 2016 Phase 2
NCT03377556 Recruiting ATM Gene Mutation|ATR Gene Mutation|BARD1 Gene Mutation|BRCA1 Gene Mutation|BRCA2 Gene Mutation|BRIP1 Gene Mutation|CHEK1 Gene Mutation|CHEK2 Gene Mutation|FANCA Gene Mutation|FANCC Gene Mutation|FANCD2 Gene Mutation|FANCF Gene Mutation|FANCM Gene Mutation|NBN Gene Mutation|PALB2 Gene Mutation|RAD51 Gene Mutation|RAD51B Gene Mutation|RAD54L Gene Mutation|Recurrent Squamous Cell Lung Carcinoma|RPA1 Gene Mutation|Stage IV Squamous Cell Lung Carcinoma AJCC v7 Southwest Oncology Group|National Cancer Institute (NCI) February 7 2017 Phase 2
NCT03077607 Completed Advanced Solid Tumors Pfizer|Medivation Inc. November 7 2016 Phase 1
NCT03148795 Recruiting Prostate Cancer Pfizer|Medivation Inc. July 4 2017 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