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Selleck该产品发表文献36篇:

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 NW\wUHlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG2NE4yNTFyMDDuUS=> MXOyOE81QC95MjDo M4n0WYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 MoD2NlYxPDd4OUe=
BR5FVB1-Akt NILpcY5CeG:ydH;zbZMhSXO|YYm= MVmwMlEuOTByIH7N MlTmO|IhcA>? M4f3Zolv\HWlZYOgZZBweHSxc3nz NWrRdZN3OjZyNEe2PVc>
Capan-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTF4LkFihKnDueLCiUWuOQKBkcL3TdMg NF3r[5czPTh4NEW5NC=>
MIA PaCa-2 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\QTWM2OD13OD6yN-KBkcLz4pEJPE4y6oDLwsXNxsA> M2HtU|I2QDZ2NUmw
RD NYr3UXZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRThwNzDuUS=> MWGyOVI3OzV|OR?=
Rh41 Mn;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRThwMTDuUS=> NEjiRpUzPTJ4M{WzPS=>
Rh18 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LMOGlEPTB;ND65JI5O MYqyOVI3OzV|OR?=
Rh30 NWLaOIhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTNzLkGgcm0> M4S3UlI2OjZ|NUO5
BT-12 MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRuLCiUGsNFAxKG6P MU[yOVI3OzV|OR?=
CHLA-266 NHq5eXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\Vb2lEPTB-4pEJNUwxODBibl2= MWiyOVI3OzV|OR?=
TC-71 NFf2c4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHaTWM2OD1|Lkegcm0> NYrs[WMyOjV{NkO1N|k>
CHLA-9 NGS4eYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DJe2lEPTB;OD6yJI5O MnSxNlUzPjN3M{m=
CHLA-10 M1vucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn2yTWM2OD14Nz64JI5O Ml3vNlUzPjN3M{m=
CHLA-258 NGKweXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrnTWM2OD12Lk[gcm0> MWSyOVI3OzV|OR?=
SJ-GBM2 M3\kPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF4LkKgcm0> MYGyOVI3OzV|OR?=
NB-1643 M2fIbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTF6LkSgcm0> NULKcpY6OjV{NkO1N|k>
NB-EBc1 MkfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTsO3U3UUN3ME2yOU45KG6P MkLiNlUzPjN3M{m=
CHLA-90 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS4NZpKSzVyPvMAjVEtODByIH7N NVi3cHVqOjV{NkO1N|k>
CHLA-136 NHvPXGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDpWYxVUUN3ME2xOE4zKG6P M1HlOlI2OjZ|NUO5
NALM-6 MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LHNmlEPTB;NEmgcm0> MVqyOVI3OzV|OR?=
COG-LL-317 MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrEbpBKSzVyPUmuOEBvVQ>? NH3ueo4zPTJ4M{WzPS=>
RS4;11 MnTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXK1[JFPUUN3ME21Nk43KG6P NVzMdZZvOjV{NkO1N|k>
MOLT-4 NYrzb5Q{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvPRmpFUUN3ME2xOk43KG6P NIPPTpkzPTJ4M{WzPS=>
CCRF-CEM NFTiS2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHK4ZZNKSzVyPU[5O{4{KG6P M1rFZlI2OjZ|NUO5
Kasumi-1 NXL6flZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;VeFFLUUN3ME23PFYvOiCwTR?= NFq1fVQzPTJ4M{WzPS=>
Karpas-299 NYXBd|BZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nlbmlEPTB;N{WuO{BvVQ>? NYfQd5Y6OjV{NkO1N|k>
Ramos-RA1 NXTUbFJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j5b2lEPTB;NkiuN{BvVQ>? NFfY[Y8zPTJ4M{WzPS=>
DT40 NYnFUZl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnaZYlKSzVyPUSgcm0> NHjGbYMzPDN3NkixNy=>
DU145 Mor4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFzIH7N M3zXO|I1OzV4OEGz
H209 M2jTeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwNzDuUS=> NX;Gbo5yOjRyN{ezOVA>
H1048 MlrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXZXmRKSzVyPUKuNkBvVQ>? MlryNlQxPzd|NUC=
H524 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrJTWM2OD1|LkGgcm0> MnP3NlQxPzd|NUC=
H1930 NIPhe4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofrTWM2OD12LkGgcm0> NUnRcmNJOjRyN{ezOVA>
H69 MoHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWmzbXprUUN3ME21MlIhdk1? MUeyOFA4PzN3MB?=
H2081 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;EcYVKSzVyPU[uN{BvVQ>? M1H1TVI1ODd5M{Ww
H2107 NY\TTpgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHX0cJpKSzVyPUeuN{BvVQ>? NH\Ee5EzPDB5N{O1NC=>
H1092 NGHVR2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rBeWlEPTB;OD65JI5O M2TNZ|I1ODd5M{Ww
DMS-79 M2HjPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\vWFZKSzVyPUmuN{BvVQ>? Ml\TNlQxPzd|NUC=
H446 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvzTWM2OD1zMzDuUS=> MoG2NlQxPzd|NUC=
COR-L279 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmntTWM2OD1zNTDuUS=> MnftNlQxPzd|NUC=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cleaved-PARP / cleaved-caspase3 / γ-H2AX; 

PubMed: 29158830     


Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W0069 cells.

pKAP1 / pChk2 / pChk1; 

PubMed: 28947502     


Western blot images (representative from 3 independent experiments) showing the impact of a 24 hour pre-treatment with TAL ± TMZ on DNA damage signaling in U251 (MGMT-low) and T98G (MGMT-high) cells. 

PD-L1; 

PubMed: 28167507     


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. 

p-ATM; 

PubMed: 30472087     


Western blot analysis of the DNA damage sensors ATM, p-ATM (Ser1981), CHK1, p-CHK1 (Ser317), CHK2 and p-CHK2 (Thr68) in MV4-11 and HL-60 cells. GAPDH served as a loading control.

29158830 28947502 28167507 30472087
Growth inhibition assay
Cell viability; 

PubMed: 29158830     


Measured dose response curve and IC50 of Talazoparib in W780 and W0069 cells.

29158830
Immunofluorescence
cleaved PARP / 53BP1; 

PubMed: 28958991     


Cleaved-PARP and 53BP1 expression. Representative images with 10× objective from high-content imaging of control cells in the left column, and cells treated with veliparib, olaparib, and talazoparib in three right columns. 53BP1 expression is seen in: A, HCC1143; B, MDAMB231; and C, HCC1806. Blue represents nuclear staining and pink foci represent 53BP1 foci. Cleaved-PARP expression is seen in D, HCC1143 and E, HCC1806. Blue represents nuclear staining and green represents cleaved-PARP expression.

RAD51; 

PubMed: 30621214     


(A) MCF7 and (B) MCF7-T cells were treated with either 100 nM tamoxifen (Tamox) or 1 nM talazoparib (Talaz) for 72 h, alone and in combination. 24 h post treatment RAD51 foci formation assay was performed. Scale bar: 20 µm.

28958991 30621214
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
储存条件 粉状
溶于溶剂
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 (mg) = 浓度 (mM) x 体积 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03974217 Recruiting Drug: Talazoparib Leukemia Dana-Farber Cancer Institute|Pfizer August 1 2019 Phase 1
NCT03901469 Recruiting Drug: ZEN003694|Drug: Talazoparib Triple Negative Breast Cancer Zenith Epigenetics|Pfizer June 26 2019 Phase 2
NCT03911973 Recruiting Drug: Gedatolisib|Drug: Talazoparib TNBC - Triple-Negative Breast Cancer Kari Wisinski|Pfizer|Big Ten Cancer Research Consortium April 17 2019 Phase 1|Phase 2
NCT03875313 Recruiting Drug: CB-839|Drug: Talazoparib Solid Tumor|Clear Cell Renal Cell Carcinoma|TNBC - Triple-Negative Breast Cancer|Colorectal Cancer|CRC|RCC|ccRCC Calithera Biosciences Inc March 22 2019 Phase 1|Phase 2
NCT03672773 Recruiting Drug: Talazoparib|Drug: Temozolomide 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

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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