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

CAS No. 1207456-01-6

Talazoparib (BMN 673, LT-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生产的Talazoparib (BMN 673)发表文献111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, LT-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 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXhXZoxNjFvMUCwJI5O MU[yOE81QC95MjDo M3\N[4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHTldIVv\GWwdHz5 NHmyPI0zPjB2N{[5Oy=>
BR5FVB1-Akt NIr0fYFCeG:ydH;zbZMhSXO|YYm= MkL5NE4yNTFyMDDuUS=> NXn4PWM2PzJiaB?= MYTpcoR2[2W|IHHwc5B1d3Orcx?= MnvRNlYxPDd4OUe=
Capan-1 M4HySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\SNmlEPTB;MU[uNQKBkcLz4pEJOU416oDLwsXNxsA> M13DUlI2QDZ2NUmw
MIA PaCa-2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TRRWlEPTB;NUiuNlPjiIoEsfMAjVgvOeLCidM1UeKh NXHTZotsOjV6NkS1PVA>
RD MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoroTWM2OD16Lkegcm0> M{LOO|I2OjZ|NUO5
Rh41 MnXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu3OoZKSzVyPUiuNUBvVQ>? MU[yOVI3OzV|OR?=
Rh18 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\6TWM2OD12Lkmgcm0> M{fvV|I2OjZ|NUO5
Rh30 M2Tzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XxcmlEPTB;M{GuNUBvVQ>? MnX5NlUzPjN3M{m=
BT-12 MmTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRuLCiUGsNFAxKG6P NIHIc4MzPTJ4M{WzPS=>
CHLA-266 MmHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrqNVBKSzVyPvMAjVEtODByIH7N M4TMRVI2OjZ|NUO5
TC-71 NGr0U4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXDNXZKSzVyPUOuO{BvVQ>? M1r1b|I2OjZ|NUO5
CHLA-9 M2LGUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jvT2lEPTB;OD6yJI5O NXPLS4g{OjV{NkO1N|k>
CHLA-10 Ml;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTZ5Lkigcm0> MkjiNlUzPjN3M{m=
CHLA-258 M1vrNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvjPYlKSzVyPUSuOkBvVQ>? M4\QUlI2OjZ|NUO5
SJ-GBM2 M1nVO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHNSIhPUUN3ME2xOk4zKG6P MmnJNlUzPjN3M{m=
NB-1643 NF3YPJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\XVXZKSzVyPUG4MlQhdk1? NGrrRnkzPTJ4M{WzPS=>
NB-EBc1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3X0TmlEPTB;MkWuPEBvVQ>? NIjmPFczPTJ4M{WzPS=>
CHLA-90 NEm2Z5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPwTWM2OD8kgJmxMFAxOCCwTR?= MXmyOVI3OzV|OR?=
CHLA-136 NXnkT41bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmKxTWM2OD1zND6yJI5O M4n4e|I2OjZ|NUO5
NALM-6 M{PrSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnsNG9KSzVyPUS5JI5O NGG2eo0zPTJ4M{WzPS=>
COG-LL-317 MmT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTlwNDDuUS=> M175cFI2OjZ|NUO5
RS4;11 MkW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;J[mlEPTB;NUKuOkBvVQ>? MmXBNlUzPjN3M{m=
MOLT-4 NUPhXHdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDvTJk6UUN3ME2xOk43KG6P M2\xRVI2OjZ|NUO5
CCRF-CEM NUWwPJVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHQTWM2OD14OUeuN{BvVQ>? NEHiXmszPTJ4M{WzPS=>
Kasumi-1 M3nJUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXxeHNKSzVyPUe4Ok4zKG6P MWmyOVI3OzV|OR?=
Karpas-299 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjGUXIxUUN3ME23OU44KG6P NX\ZWGhKOjV{NkO1N|k>
Ramos-RA1 MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTZ6LkOgcm0> NVT2e|VkOjV{NkO1N|k>
DT40 Mn;LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r3dmlEPTB;NDDuUS=> NHfiVpMzPDN3NkixNy=>
DU145 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fnVGlEPTB;MUGgcm0> NUX4c4x7OjR|NU[4NVM>
H209 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzIR4dSUUN3ME2xMlchdk1? M4PPZVI1ODd5M{Ww
H1048 MlzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\ie5NYUUN3ME2yMlIhdk1? MY[yOFA4PzN3MB?=
H524 NUK2R2M4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEX2THBKSzVyPUOuNUBvVQ>? MX:yOFA4PzN3MB?=
H1930 NXHGXmVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\ZTWM2OD12LkGgcm0> MVKyOFA4PzN3MB?=
H69 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTVwMjDuUS=> NYflTpBwOjRyN{ezOVA>
H2081 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7xTWM2OD14LkOgcm0> MnHKNlQxPzd|NUC=
H2107 M{jwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTdwMzDuUS=> NYTNZnU{OjRyN{ezOVA>
H1092 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTwTWM2OD16Lkmgcm0> NFexdpczPDB5N{O1NC=>
DMS-79 NF:yc4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofVTWM2OD17LkOgcm0> NX;nNnpmOjRyN{ezOVA>
H446 NEXLd2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLpeZFKSzVyPUGzJI5O MnrINlQxPzd|NUC=
COR-L279 NHe4TGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnPTWM2OD1zNTDuUS=> NH:wNlEzPDB5N{O1NC=>

... 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(配方适用于不溶于水的药物;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
NCT04497116 Recruiting Drug: RP-3500|Drug: Talazoparib: oral PARP inhibitor Advanced Solid Tumor Adult Repare Therapeutics July 22 2020 Phase 1|Phase 2
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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID