Talazoparib (BMN 673)

别名: LT-673 中文名称:他拉唑帕利

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。

Talazoparib (BMN 673) Chemical Structure

Talazoparib (BMN 673) Chemical Structure

CAS: 1207456-01-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 794.43 现货
10mg RMB 1040.13 现货
50mg RMB 3104.01 现货
200mg RMB 24324.3 现货
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客户使用Selleck的Talazoparib (BMN 673)发表文献213

产品质控

批次: 纯度: 99.84%
99.05

Talazoparib (BMN 673)相关产品

相关信号通路图

PARP抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
BR5FVB1-Akt Apoptosis Assay 0.1-100 nM 72 h induces apoptosis 26047697
BR5FVB1-Akt Growth Inhibition Assay 0.1-100 nM 24/48/72 h inhibits cell proliferation dose dependently 26047697
LoVo Cytotoxicity assay 0.4 uM 5 days GI50 = 0.004 μM 26652717
MX1 Function assay 1 mg/kg 2 ,8 and 24 hrs Decrease in PAR level in athymic nu/nu mouse xenografted with human MX1 cells at 1 mg/kg, po administered as single dose measured after 2 ,8 and 24 hrs by ELISA 26652717
MX1 Antitumor assay 0.33 mg/kg 28 days Antitumor activity against BRCA1 deficient human MX1 cells xenografted in athymic nu/nu mouse at 0.33 mg/kg, po qd administered for 28 days 26652717
MX1 Antitumor assay 0.165 mg/kg 28 days Antitumor activity against BRCA1 deficient human MX1 cells xenografted in athymic nu/nu mouse assessed as tumor growth inhibition at 0.165 mg/kg, po administered twice a day for 28 days 26652717
Capan1 Function assay 0.1 uM 4 hrs Inhibition of PARP1 in BRCA2 deficient human Capan1 cells assessed as increase in PARP1-DNA trapping at 0.1 uM after 4 hrs by Western blot analysis 28692916
MDA-MB-436 Function assay 1 uM 4 hrs Inhibition of PARP1 in BRCA1 deficient human MDA-MB-436 cells assessed as increase in PARP1-DNA trapping at 1 uM after 4 hrs by Western blot analysis 28692916
MX1 Function assay 0.33 mg/kg Potentiation of carboplatin-induced tumor growth inhibition of BRCA1 deficient human MX1 cells xenografted in athymic nu/nu mouse at 0.33 mg/kg po and animals were treated with carboplatin at 35 mg/kg, ip on day 1 26652717
LoVo Function assay 30 mins EC50 = 0.0025 μM 25761096
LoVo Function assay 30 mins EC50 = 0.00251 μM 26652717
MDA-MB-436 Antiproliferative assay 7 days IC50 = 0.0007 μM 28692916
Capan1 Antiproliferative assay 7 days IC50 = 0.0018 μM 28692916
VC8 Cytotoxicity assay 3 days IC50 = 0.0042 μM 28692916
V79 Cytotoxicity assay 3 days IC50 = 5.0114 μM 28692916
NALM-6 Growth Inhibition Assay IC50=49 nM 25263539
CHLA-136 Growth Inhibition Assay IC50=14.2 nM 25263539
CHLA-90 Growth Inhibition Assay IC50> 1,000 nM 25263539
NB-EBc1 Growth Inhibition Assay IC50=25.8 nM 25263539
NB-1643 Growth Inhibition Assay IC50=18.4 nM 25263539
SJ-GBM2 Growth Inhibition Assay IC50=16.2 nM 25263539
CHLA-258 Growth Inhibition Assay IC50=4.6 nM 25263539
CHLA-10 Growth Inhibition Assay IC50=67.8 nM 25263539
CHLA-9 Growth Inhibition Assay IC50=8.2 nM 25263539
TC-71 Growth Inhibition Assay IC50=3.7 nM 25263539
CHLA-266 Growth Inhibition Assay IC50> 1,000 nM 25263539
BT-12 Growth Inhibition Assay IC50> 1,000 nM 25263539
Rh30 Growth Inhibition Assay IC50=31.1 nM 25263539
Rh18 Growth Inhibition Assay IC50=4.9 nM 25263539
Rh41 Growth Inhibition Assay IC50=8.1 nM 25263539
RD Growth Inhibition Assay IC50=8.7 nM 25263539
MIA PaCa-2 Growth Inhibition Assay IC50=58.23 ± 8.1 µM  25864590
Capan-1 Growth Inhibition Assay IC50=16.0 ± 5.4 µM  25864590
COG-LL-317 Growth Inhibition Assay IC50=9.4 nM 25263539
RS4;11 Growth Inhibition Assay IC50=52.6 nM 25263539
MOLT-4 Growth Inhibition Assay IC50=16.6 nM 25263539
CCRF-CEM Growth Inhibition Assay IC50=697.3 nM 25263539
Kasumi-1 Growth Inhibition Assay IC50=786.2 nM 25263539
Karpas-299 Growth Inhibition Assay IC50=75.7 nM 25263539
Ramos-RA1 Growth Inhibition Assay IC50=68.3 nM 25263539
DT40 Growth Inhibition Assay IC50=4 nM 24356813
DU145 Growth Inhibition Assay IC50=11 nM 24356813
H209 Growth Inhibition Assay IC50=1.7 nM 24077350
H1048 Growth Inhibition Assay IC50=2.2 nM 24077350
H524 Growth Inhibition Assay IC50=3.1 nM 24077350
H1930 Growth Inhibition Assay IC50=4.1 nM 24077350
H69 Growth Inhibition Assay IC50=5.2 nM 24077350
H2081 Growth Inhibition Assay IC50=6.3 nM 24077350
H2107 Growth Inhibition Assay IC50=7.3 nM 24077350
H1092 Growth Inhibition Assay IC50=8.9 nM 24077350
DMS-79 Growth Inhibition Assay IC50=9.3 nM 24077350
H446 Growth Inhibition Assay IC50=13 nM 24077350
COR-L279 Growth Inhibition Assay IC50=15 nM 24077350
MX1 Cytotoxicity assay EC50 = 0.0003 μM 26652717
Capan1 Cytotoxicity assay EC50 = 0.005 μM 26652717
MRC5 Cytotoxicity assay EC50 = 0.31 μM 26652717
点击查看更多细胞系数据

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(In Vitro)
体外研究活性

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]

实验图片 检测方法 检测指标 实验图片 PMID
Western blot pKAP1 / pChk2 / pChk1 cleaved-PARP / cleaved-caspase3 / γ-H2AX p-ATM PD-L1 28947502
Growth inhibition assay Cell viability 29158830
Immunofluorescence cleaved PARP / 53BP1 RAD51 28958991
体内研究(In Vivo)
体内研究活性

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]

动物实验 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05425862 Suspended
Metastatic Castration Resistant Prostate Cancer (mCRPC)
Peter MacCallum Cancer Centre Australia
October 21 2022 Phase 1
NCT05141708 Completed
Metastatic Breast Cancer|Breast Neoplasms
Pfizer
December 17 2021 --
NCT05053854 Recruiting
Neuroendocrine Tumors
Peter MacCallum Cancer Centre Australia
December 8 2021 Phase 1
NCT04991480 Active not recruiting
Advanced Cancer|Metastatic Cancer|Breast Cancer
Artios Pharma Ltd
September 13 2021 Phase 1|Phase 2
NCT04987931 Completed
Breast Cancer
Pfizer
August 20 2021 --

化学信息&溶解度

分子量 380.35 分子式

 

C19H14F2N6O
 
CAS号 1207456-01-6 SDF --
Smiles CN1C(=NC=N1)C2C(NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 76 mg/mL ( 199.81 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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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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