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IC50为0.58 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. 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IC50为0.58 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
PARP [1]
(Cell-free assay)
0.58 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 NYX6XI4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUWwMlEuOTByIH7N NV[2ZXBvOjRxNEivO|IhcA>? NVXxRmRtcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> Mn[yNlYxPDd4OUe=
BR5FVB1-Akt MnXwRZBweHSxc3nzJGF{e2G7 NHH2e3AxNjFvMUCwJI5O NVnHNWw2PzJiaB?= M4Cz[Ylv\HWlZYOgZZBweHSxc3nz MWeyOlA1PzZ7Nx?=
Capan-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\KVm9KSzVyPUG2MlDjiIoEsfMAjVUvPOLCidM1UeKh M{jJNlI2QDZ2NUmw
MIA PaCa-2 Mk[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmP3TWM2OD13OD6yN-KBkcLz4pEJPE4y6oDLwsXNxsA> NHPhN3YzPTh4NEW5NC=>
RD MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi0clhKSzVyPUiuO{BvVQ>? MYqyOVI3OzV|OR?=
Rh41 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K0[WlEPTB;OD6xJI5O NH3adlgzPTJ4M{WzPS=>
Rh18 MkP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTRwOTDuUS=> M2TjbFI2OjZ|NUO5
Rh30 NEXqfWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1e3fmlEPTB;M{GuNUBvVQ>? MVGyOVI3OzV|OR?=
BT-12 MmLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PCTGlEPTB-4pEJNUwxODBibl2= Ml3CNlUzPjN3M{m=
CHLA-266 MmjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37T[2lEPTB-4pEJNUwxODBibl2= NYXkeFRpOjV{NkO1N|k>
TC-71 NFLCcpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzpU4gyUUN3ME2zMlchdk1? MYiyOVI3OzV|OR?=
CHLA-9 MmTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVqzbXI2UUN3ME24MlIhdk1? MVGyOVI3OzV|OR?=
CHLA-10 M2HXZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L3RWlEPTB;NkeuPEBvVQ>? MkPUNlUzPjN3M{m=
CHLA-258 M1HRVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTRwNjDuUS=> MXmyOVI3OzV|OR?=
SJ-GBM2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3MfFJTUUN3ME2xOk4zKG6P MkXkNlUzPjN3M{m=
NB-1643 NIKwU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2O0UmlEPTB;MUiuOEBvVQ>? Mn:5NlUzPjN3M{m=
NB-EBc1 NHvocGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnBTWM2OD1{NT64JI5O Moq3NlUzPjN3M{m=
CHLA-90 MljHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVG4PWI3UUN3ME9ihKkyNDByMDDuUS=> MoftNlUzPjN3M{m=
CHLA-136 NX7OeHhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LaXGlEPTB;MUSuNkBvVQ>? MoHiNlUzPjN3M{m=
NALM-6 NH;N[XFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTR7IH7N M1LlT|I2OjZ|NUO5
COG-LL-317 NFTyTIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLCTWM2OD17LkSgcm0> M1f4blI2OjZ|NUO5
RS4;11 MmriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTV{Lk[gcm0> Ml\PNlUzPjN3M{m=
MOLT-4 NYHWVHY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rWOGlEPTB;MU[uOkBvVQ>? MnHoNlUzPjN3M{m=
CCRF-CEM NEnDNpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVmxZ5I6UUN3ME22PVcvOyCwTR?= MonFNlUzPjN3M{m=
Kasumi-1 NWTJVIRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M133dWlEPTB;N{i2MlIhdk1? MmXSNlUzPjN3M{m=
Karpas-299 MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTd3Lkegcm0> MnT6NlUzPjN3M{m=
Ramos-RA1 M3fxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXCfoxzUUN3ME22PE4{KG6P MmjQNlUzPjN3M{m=
DT40 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\rTWM2OD12IH7N NWn4eVlXOjR|NU[4NVM>
DU145 NHLscGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWiyOY03UUN3ME2xNUBvVQ>? M{HYWVI1OzV4OEGz
H209 NYTsbJh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTFwNzDuUS=> NUTJOHBFOjRyN{ezOVA>
H1048 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTJwMjDuUS=> M13GO|I1ODd5M{Ww
H524 M1;5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;JSolVUUN3ME2zMlEhdk1? M1XIflI1ODd5M{Ww
H1930 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTRwMTDuUS=> MYOyOFA4PzN3MB?=
H69 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXXenNKSzVyPUWuNkBvVQ>? NFfOPYczPDB5N{O1NC=>
H2081 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\BN3RKSzVyPU[uN{BvVQ>? MXOyOFA4PzN3MB?=
H2107 M4DXVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;OfHpKSzVyPUeuN{BvVQ>? NILScFAzPDB5N{O1NC=>
H1092 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;4WGlEPTB;OD65JI5O MYqyOFA4PzN3MB?=
DMS-79 NHPmNolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LDZmlEPTB;OT6zJI5O M3v1WlI1ODd5M{Ww
H446 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHlTWM2OD1zMzDuUS=> NF7Q[lAzPDB5N{O1NC=>
COR-L279 Mn\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HUO2lEPTB;MUWgcm0> NHv6OWIzPDB5N{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
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"

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID