BMN-673 8R,9S
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BMN-673 8R,9S 是一种BMN-673的无活性构型,可用于阴性对照实验。
PARP1/2抑制剂是一类靶向DNA修复中肿瘤特异性缺陷的抗癌剂。BMN 673是一种高度有效的PARP1/2抑制剂。
体外:BMN 673是一种强效的PARP1/2抑制剂,但不抑制测试的其他酶。BMN 673显示出选择性的抗肿瘤细胞毒性,并且在比上一代PARP1/2抑制剂更小的浓度下产生DNA损伤修复生物标记物。BMN 673体外选择性地靶向BRCA1、BRCA2或PTEN基因缺陷的肿瘤细胞,效力比现有的PARP1/2抑制剂强20到200多倍 [1]。
体内: BMN 673易口服且具有生物利用度,大鼠CMC给药具有40%以上的绝对口服生物利用度。口服BMN 673引起小鼠显著的抗肿瘤活性;携带BRCA基因突变或PTEN缺陷导致的DNA修复缺陷的异种移植瘤对良好耐受剂量的口服BMN 673治疗十分敏感。BMN 673与替莫唑胺、SN38或铂药物联合用药时,具有协同抗肿瘤效果[1]。
临床试验:在3-6例患者(pts)/剂量水平的2阶段剂量递增研究中,对BMN 673的药代动力学(PK)、药效学(PD)、安全性和抗肿瘤活性进行了评价。结果表明,在带有BRCA 突变的患者中,由于剂量限制性血小板减少症,使用II期临床试验推荐剂量1000 μg/d的单剂,BMN 673耐受性良好,具有良好的抗肿瘤活性。
参考文献:
[1] Shen Y, Rehman FL, Feng Y, Boshuizen J, Bajrami I, Elliott R, Wang B, Lord CJ, Post LE, Ashworth A. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res. 2013;19(18):5003-15.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 380.35 |
Cas No. | 1207456-00-5 |
Formula | C19H14F2N6O |
Synonyms | (8R,9S)-BMN-673 |
Solubility | ≥38 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥15.03 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | (8R,9S)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one |
SDF | Download SDF |
Canonical SMILES | O=C1C2=CC(F)=CC(N[C@@H](C3=CC=C(F)C=C3)[C@@H]4C5=NC=NN5C)=C2C4=NN1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
BMN-673 8R,9S is an inactive form of BMN 673 and can be used as negative control. | ||||||
Targets | ||||||
IC50 |
质量控制和MSDS
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