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 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfVWGwxNjFvMUCwJI5O MUKyOE81QC95MjDo NYf1PFZkcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NX;RWVJPOjZyNEe2PVc>
BR5FVB1-Akt Ml\SRZBweHSxc3nzJGF{e2G7 M4\tflAvOS1zMECgcm0> NVvxXYU1PzJiaB?= M1nUdYlv\HWlZYOgZZBweHSxc3nz NV\KTppjOjZyNEe2PVc>
Capan-1 Mmi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TyT2lEPTB;MU[uNQKBkcLz4pEJOU416oDLwsXNxsA> NELJXnYzPTh4NEW5NC=>
MIA PaCa-2 M3HKW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTV6LkKz5qCKyrIkgJm4MlHjiIoEtV5CpC=> M{D3VlI2QDZ2NUmw
RD NYPVXIZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRThwNzDuUS=> M1HzdVI2OjZ|NUO5
Rh41 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV2wPXZ6UUN3ME24MlEhdk1? MlTnNlUzPjN3M{m=
Rh18 M13pUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrvTWM2OD12Lkmgcm0> NXHHOo45OjV{NkO1N|k>
Rh30 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zOeWlEPTB;M{GuNUBvVQ>? M1L5PFI2OjZ|NUO5
BT-12 M1fKNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLseWJZUUN3ME9ihKkyNDByMDDuUS=> Mo\xNlUzPjN3M{m=
CHLA-266 M1vCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\iTWM2OD8kgJmxMFAxOCCwTR?= NGq4fGMzPTJ4M{WzPS=>
TC-71 NWPGOpVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f2RWlEPTB;Mz63JI5O M{PhNVI2OjZ|NUO5
CHLA-9 MmLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPpTWM2OD16LkKgcm0> MlXVNlUzPjN3M{m=
CHLA-10 M13t[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXa[4tKSzVyPU[3Mlghdk1? NHzG[2UzPTJ4M{WzPS=>
CHLA-258 M2fPVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVT4fFE4UUN3ME20MlYhdk1? M2HBTVI2OjZ|NUO5
SJ-GBM2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\UV5hrUUN3ME2xOk4zKG6P MWGyOVI3OzV|OR?=
NB-1643 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\yTWM2OD1zOD60JI5O NVzEPXl{OjV{NkO1N|k>
NB-EBc1 MkTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV:zW5NDUUN3ME2yOU45KG6P MlTpNlUzPjN3M{m=
CHLA-90 Mkm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRuLCiUGsNFAxKG6P MUeyOVI3OzV|OR?=
CHLA-136 NWDESpUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTF2LkKgcm0> NUDMVm94OjV{NkO1N|k>
NALM-6 MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\lSWlEPTB;NEmgcm0> Mn63NlUzPjN3M{m=
COG-LL-317 MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{H4eGlEPTB;OT60JI5O MUWyOVI3OzV|OR?=
RS4;11 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTV{Lk[gcm0> M3\RUlI2OjZ|NUO5
MOLT-4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHm5fIdKSzVyPUG2MlYhdk1? NUPDR5UxOjV{NkO1N|k>
CCRF-CEM M3rMZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jnR2lEPTB;Nkm3MlMhdk1? M37vdFI2OjZ|NUO5
Kasumi-1 M1vScWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTd6Nj6yJI5O MYWyOVI3OzV|OR?=
Karpas-299 NUj5cmFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW2elAzUUN3ME23OU44KG6P NUTLV4hLOjV{NkO1N|k>
Ramos-RA1 NUDCPGFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPjbIJKSzVyPU[4MlMhdk1? NWLDU5ZWOjV{NkO1N|k>
DT40 NUO5NYQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLsTWM2OD12IH7N NXLhcHdOOjR|NU[4NVM>
DU145 Mn72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHtTWM2OD1zMTDuUS=> MYOyOFM2PjhzMx?=
H209 NWDKWnFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Dv[WlEPTB;MT63JI5O NYjocZRTOjRyN{ezOVA>
H1048 NEXacnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;KZlAzUUN3ME2yMlIhdk1? MUOyOFA4PzN3MB?=
H524 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTNwMTDuUS=> M4f3XVI1ODd5M{Ww
H1930 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TzfWlEPTB;ND6xJI5O Ml2xNlQxPzd|NUC=
H69 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3vW2JYUUN3ME21MlIhdk1? M4XGRVI1ODd5M{Ww
H2081 Mn3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTyTWM2OD14LkOgcm0> NWXLN|hROjRyN{ezOVA>
H2107 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITkOYJKSzVyPUeuN{BvVQ>? MlW3NlQxPzd|NUC=
H1092 NHX5WVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRThwOTDuUS=> MWeyOFA4PzN3MB?=
DMS-79 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr5N3hpUUN3ME25MlMhdk1? NUKyR2M{OjRyN{ezOVA>
H446 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTF|IH7N NEjoUZMzPDB5N{O1NC=>
COR-L279 MmTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T3eGlEPTB;MUWgcm0> NWewOlFxOjRyN{ezOVA>

... 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
NCT01989546 Active, not recruiting Advanced Ovarian Cancer|Primary Peritoneal Cancer|Advanced Breast Cancer|Advanced Solid Tumors National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) November 8, 2013 Phase 1|Phase 2
NCT02286687 Active, not recruiting Advanced Cancers M.D. Anderson Cancer Center|BioMarin Pharmaceutical December 22, 2014 Phase 2
NCT02997163 Not yet recruiting Advanced Solid Tumors Medivation, Inc. January 2017 Phase 1
NCT02997176 Recruiting Advanced Solid Tumors Medivation, Inc. November 2016 Phase 1
NCT03042910 Recruiting Solid Tumor Medivation, Inc. October 2016 Phase 1
NCT02836028 Withdrawn Ovarian Cancer Medivation, Inc.|Myriad Genetic Laboratories, Inc. October 2016 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