- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實驗
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細胞核與細胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 新產(chǎn)品
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Talazoparib (BMN-673)
別名: LT-673
Talazoparib (BMN 673, LT-673)是一種新型的PARP抑制劑，無細胞試驗中對PARP1的IC50為0.57 nM。它也是有效的PARP-2抑制劑，但不抑制PARG，對PTEN突變型高度敏感。Phase 3。
Talazoparib (BMN-673) Chemical Structure
CAS: 1207456-01-6
產(chǎn)品質(zhì)控
批次：
純度：
99.88%
99.88
Talazoparib (BMN-673)相關(guān)產(chǎn)品
| 相關(guān)靶點 | PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | XAV-939 Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib 3-Aminobenzamide ME0328 NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide NU1025 BGP-15 2HCl Picolinamide BYK204165 Fluzoparib (SHR-3162) | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 凋亡分子化合物庫 DNA損傷/ DNA修復(fù)化合物庫 細胞周期化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Talazoparib (BMN 673, LT-673)是一種新型的PARP抑制劑，無細胞試驗中對PARP1的IC50為0.57 nM。它也是有效的PARP-2抑制劑，但不抑制PARG，對PTEN突變型高度敏感。Phase 3。 | ||
|---|---|---|---|
| 特性 | 到目前為止報道的最有效的選擇性PARP抑制劑。 | ||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | BMN-673 選擇性與PARP 結(jié)合，且抑制PARP-介導(dǎo)的通過堿基切除修復(fù)途徑的單鏈DNA斷裂的修復(fù)。增強了DNA鏈斷裂的積累，促進基因組不穩(wěn)定性，并最終導(dǎo)致細胞凋亡。BMN 673選擇性殺死BRCA-1或BRCA-2突變的癌細胞。BMN 673作用于BRCA-1突變 (MX-1,IC50 = 0.3 nM) 和BRCA-2 突變的細胞(Capan-1,IC50 = 5 nM)，具有單藥細胞毒性。相反, BMN-673 作用于MRC-5正常人類成纖維細胞和其他含野生型BRCA-1 和 BRCA-2基因的腫瘤細胞系，IC50為90 nM到1.9 μM。[1]
|
|||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | 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 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在大鼠的藥代動力學(xué)研究中，BMN673每天單獨給藥，具有>50％口服生物有效性和藥代動力學(xué)特性。在MX-1移植瘤腫瘤模型研究中, BMN 673每天口服給藥，顯著增強細胞毒性療法的抗腫瘤效果，這種作用具有劑量依賴性。[2] |
|
|---|---|---|
| 動物實驗 | Animal Models | MX-1模型(BRCA-1缺陷的) |
| Dosages | 0.33 mg/kg/day,每天一次 | |
| Administration | 口服處理 | |
| 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 | -- |
|
化學(xué)信息&溶解度
| 分子量 | 380.35 | 分子式 |
C19H14F2N6O
|
| CAS號 | 1207456-01-6 | SDF | -- |
| Smiles | CN1C(=NC=N1)C2C(NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 19 mg/mL ( (49.95 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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* 必填項
常見問題及建議解決方法
問題 1:
Which solvent do you recommend to dilute it for in vivo study in mice?
回答：
According to the paper: http://clincancerres.aacrjournals.org/content/19/18/5003.full, it can be dissolved in vehicle (10% DMAc, 6% Solutol, and 84% PBS). 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"
