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 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 NF;5eW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\FWVAvOS1zMECgcm0> Ml\QNlQwPDhxN{KgbC=> NUPjPYtZcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NUPCcWlNOjZyNEe2PVc>
BR5FVB1-Akt M1PSPGFxd3C2b4Ppd{BCe3OjeR?= MnmwNE4yNTFyMDDuUS=> M1r4O|czKGh? NUDTc5Q4cW6mdXPld{BieG:ydH;zbZM> MV[yOlA1PzZ7Nx?=
Capan-1 NYm4SGgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLRTWM2OD1zNj6w5qCKyrIkgJm1MlTjiIoEtV5CpC=> MWCyOVg3PDV7MB?=
MIA PaCa-2 NVzBdYhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf2T5lKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>? MWOyOVg3PDV7MB?=
RD MnvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nJe2lEPTB;OD63JI5O NVnF[VkxOjV{NkO1N|k>
Rh41 NX7Lb203T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\ETWM2OD16LkGgcm0> NHjwXJMzPTJ4M{WzPS=>
Rh18 NInWdHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHLd2pbUUN3ME20Mlkhdk1? M3SyOlI2OjZ|NUO5
Rh30 M1T2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTrTWM2OD1|MT6xJI5O M12xPVI2OjZ|NUO5
BT-12 M1y3fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRuLCiUGsNFAxKG6P MmDVNlUzPjN3M{m=
CHLA-266 NX6xNJlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Tzc2lEPTB-4pEJNUwxODBibl2= NIftfpAzPTJ4M{WzPS=>
TC-71 MkS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP6W4JKSzVyPUOuO{BvVQ>? Mmj3NlUzPjN3M{m=
CHLA-9 NUfmdVVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHSO4xKSzVyPUiuNkBvVQ>? Mm\yNlUzPjN3M{m=
CHLA-10 M3PXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rad2lEPTB;NkeuPEBvVQ>? M3LRZ|I2OjZ|NUO5
CHLA-258 NX7RW4JKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v2R2lEPTB;ND62JI5O MlHZNlUzPjN3M{m=
SJ-GBM2 NHr2ZppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3sNndKSzVyPUG2MlIhdk1? MnrHNlUzPjN3M{m=
NB-1643 MmjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13CXGlEPTB;MUiuOEBvVQ>? NHW5WYkzPTJ4M{WzPS=>
NB-EBc1 NYrzNHh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;0R5BKSzVyPUK1Mlghdk1? MoXZNlUzPjN3M{m=
CHLA-90 MlPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PNOGlEPTB-4pEJNUwxODBibl2= MX2yOVI3OzV|OR?=
CHLA-136 MmDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV6xW5pkUUN3ME2xOE4zKG6P MXGyOVI3OzV|OR?=
NALM-6 MljZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGewPXZKSzVyPUS5JI5O Mn3PNlUzPjN3M{m=
COG-LL-317 NYrONoVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3z1NWlEPTB;OT60JI5O NFvmc5YzPTJ4M{WzPS=>
RS4;11 NEfUSGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVOxZnBYUUN3ME21Nk43KG6P MkGyNlUzPjN3M{m=
MOLT-4 M1vvPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFToOGZKSzVyPUG2MlYhdk1? M1;n[|I2OjZ|NUO5
CCRF-CEM NWriRm1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle2TWM2OD14OUeuN{BvVQ>? NV33foEzOjV{NkO1N|k>
Kasumi-1 M{XKZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTd6Nj6yJI5O MXyyOVI3OzV|OR?=
Karpas-299 Mn;vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HsdWlEPTB;N{WuO{BvVQ>? NV;VfGJ6OjV{NkO1N|k>
Ramos-RA1 MoPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTZ6LkOgcm0> MYeyOVI3OzV|OR?=
DT40 NHXOdW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe5PY1KSzVyPUSgcm0> MYWyOFM2PjhzMx?=
DU145 M3jsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjpVVFyUUN3ME2xNUBvVQ>? MmTPNlQ{PTZ6MUO=
H209 NXTDZ49VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7iTWM2OD1zLkegcm0> M2LhXVI1ODd5M{Ww
H1048 MlPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPSUlZXUUN3ME2yMlIhdk1? NVr1VGRZOjRyN{ezOVA>
H524 NIq5eIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXflPXJzUUN3ME2zMlEhdk1? MUKyOFA4PzN3MB?=
H1930 MkjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfuTWM2OD12LkGgcm0> M4nMS|I1ODd5M{Ww
H69 M{juUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTVwMjDuUS=> NWHpfG5MOjRyN{ezOVA>
H2081 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjYPVJwUUN3ME22MlMhdk1? MlThNlQxPzd|NUC=
H2107 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXiTWM2OD15LkOgcm0> M2r3OlI1ODd5M{Ww
H1092 M2H2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rxeWlEPTB;OD65JI5O M3L2eFI1ODd5M{Ww
DMS-79 NX7S[otZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvGTWM2OD17LkOgcm0> NXu1Z5lHOjRyN{ezOVA>
H446 MmjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\vWpRKSzVyPUGzJI5O Mk\HNlQxPzd|NUC=
COR-L279 M1y4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX70W2ZmUUN3ME2xOUBvVQ>? M3rofFI1ODd5M{Ww

... 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