Talazoparib (BMN 673)

For research use only. Not for use in humans.

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。

规格 价格 库存 购买数量  
RMB 3831.14 现货
RMB 7944.13 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Talazoparib (BMN 673)发表文献91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 NIn2R2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{P0SlAvOS1zMECgcm0> MYGyOE81QC95MjDo NUTBfFZ2cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NVTWSHFuOjZyNEe2PVc>
BR5FVB1-Akt MXPBdI9xfG:|aYOgRZN{[Xl? M3m4UVAvOS1zMECgcm0> MWW3NkBp M2LCPIlv\HWlZYOgZZBweHSxc3nz NVfvOmR4OjZyNEe2PVc>
Capan-1 Mlu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:3TlNKSzVyPUG2MlDjiIoEsfMAjVUvPOLCidM1UeKh NWLFTldrOjV6NkS1PVA>
MIA PaCa-2 Ml;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3yU|ZKSzVyPUW4MlI{6oDLwsJihKk5NjIkgJpCuW3DqA>? M2\kelI2QDZ2NUmw
RD NHyxR5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojxTWM2OD16Lkegcm0> MmrNNlUzPjN3M{m=
Rh41 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRThwMTDuUS=> NEfzUGQzPTJ4M{WzPS=>
Rh18 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37l[mlEPTB;ND65JI5O NFjBZ3YzPTJ4M{WzPS=>
Rh30 M2L2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\L[5FKSzVyPUOxMlEhdk1? M3naRlI2OjZ|NUO5
BT-12 NX62XnRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWX1U4JNUUN3ME9ihKkyNDByMDDuUS=> M3zwNVI2OjZ|NUO5
CHLA-266 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;ocHJ2UUN3ME9ihKkyNDByMDDuUS=> MlvvNlUzPjN3M{m=
TC-71 M2TSWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDYc4RGUUN3ME2zMlchdk1? M{HJOFI2OjZ|NUO5
CHLA-9 NWHCSm9[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW[zZ2VCUUN3ME24MlIhdk1? NXu2N|FbOjV{NkO1N|k>
CHLA-10 NFnPPZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV25Z25EUUN3ME22O{45KG6P NFjuRYwzPTJ4M{WzPS=>
CHLA-258 NXrKNXl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFX1OYZKSzVyPUSuOkBvVQ>? NY\qZm45OjV{NkO1N|k>
SJ-GBM2 MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGm5VW5KSzVyPUG2MlIhdk1? NEfvU3AzPTJ4M{WzPS=>
NB-1643 NWraTmk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\PTZA{UUN3ME2xPE41KG6P NYHSXnU1OjV{NkO1N|k>
NB-EBc1 M3jJZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\j[nBLUUN3ME2yOU45KG6P NHHrXXIzPTJ4M{WzPS=>
CHLA-90 M4Dh[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRuLCiUGsNFAxKG6P NEjoPFQzPTJ4M{WzPS=>
CHLA-136 NUfHNpZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFywRVRKSzVyPUG0MlIhdk1? NYL3b21GOjV{NkO1N|k>
NALM-6 M4jYbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnp[Jl3UUN3ME20PUBvVQ>? NEfMbGszPTJ4M{WzPS=>
COG-LL-317 M1fifmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M333bWlEPTB;OT60JI5O NVjzXZJ1OjV{NkO1N|k>
RS4;11 NGDzVIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\4UVdKSzVyPUWyMlYhdk1? MX:yOVI3OzV|OR?=
MOLT-4 NHrrSHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LCeGlEPTB;MU[uOkBvVQ>? M{XzVlI2OjZ|NUO5
CCRF-CEM M1nn[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfoTWM2OD14OUeuN{BvVQ>? MYmyOVI3OzV|OR?=
Kasumi-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PISGlEPTB;N{i2MlIhdk1? NIPS[5EzPTJ4M{WzPS=>
Karpas-299 NInhNFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzYOZdKSzVyPUe1Mlchdk1? M1\ybFI2OjZ|NUO5
Ramos-RA1 M4[0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M164ZWlEPTB;NkiuN{BvVQ>? MmXyNlUzPjN3M{m=
DT40 Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPjTWM2OD12IH7N MXqyOFM2PjhzMx?=
DU145 M1jTeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFzIH7N NUXUS3g{OjR|NU[4NVM>
H209 MmHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWX3WFFNUUN3ME2xMlchdk1? NV3nVHA6OjRyN{ezOVA>
H1048 NX35bnVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\LZmJKSzVyPUKuNkBvVQ>? MkDwNlQxPzd|NUC=
H524 NHu0NYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXeyRWdMUUN3ME2zMlEhdk1? M1TBW|I1ODd5M{Ww
H1930 NFHRWYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfzOZBkUUN3ME20MlEhdk1? MWOyOFA4PzN3MB?=
H69 MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTVwMjDuUS=> NIS5bFEzPDB5N{O1NC=>
H2081 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnOyTWM2OD14LkOgcm0> NVPwSYk5OjRyN{ezOVA>
H2107 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTuUZdYUUN3ME23MlMhdk1? MnvJNlQxPzd|NUC=
H1092 M37SVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH22cJRKSzVyPUiuPUBvVQ>? M4T3PVI1ODd5M{Ww
DMS-79 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTUTWM2OD17LkOgcm0> M1iwfFI1ODd5M{Ww
H446 NYHJS2cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjl[FRIUUN3ME2xN{BvVQ>? MWGyOFA4PzN3MB?=
COR-L279 M{nk[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37WfGlEPTB;MUWgcm0> MkP5NlQxPzd|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]

- 合并
  • Animal Models: MX-1模型(BRCA-1缺陷的)
  • 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

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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
NCT04337970 Recruiting Drug: Talazoparib|Drug: Axitinib Kidney Cancer|Renal Cell Carcinoma|Unresectable Renal Cell Carcinoma|Metastatic Renal Cell Carcinoma Memorial Sloan Kettering Cancer Center April 6 2020 Phase 1|Phase 2
NCT04134884 Recruiting Drug: Talazoparib|Drug: ASTX727 Metastatic Breast Cancer|Triple Negative Breast Cancer|Hormone Receptor Positive Tumor Kathy Miller|Pfizer|Astex Pharmaceuticals Inc.|Van Andel Institute Stand Up to Cancer Team|Indiana University March 30 2020 Phase 1
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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

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

相关PARP产品

Tags: 购买Talazoparib (BMN 673) | Talazoparib (BMN 673)供应商 | 采购Talazoparib (BMN 673) | Talazoparib (BMN 673)价格 | Talazoparib (BMN 673)生产 | 订购Talazoparib (BMN 673) | Talazoparib (BMN 673)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID