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1436391-86-4
  • names:

    PF-06380101

  • CAS号:

    1436391-86-4

    MDL Number: No data available
  • MF(分子式): C39H62N6O6S MW(分子量): 743.01
  • EINECS:No data available Reaxys Number:No data available
  • Pubchem ID:71569947 Brand:BIOFOUNT
PF-06380101
PF-06380101(1436391-86-4,AUR-0101)是一种微管抑制剂,PF-06380101具有强细胞毒性,PF-06380101是新型的细胞毒性Dolastatin 10类似物,PF-06380101与用于ADC制备的其他合成澳瑞他汀类似物相比,在肿瘤细胞增殖测定中具有出色的功效,并且具有不同的ADME特性。
货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
YZM000915-5mg 5mg 99.6% ¥ 3543.00 ¥ 3543.00 2-3天
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¥ 0.00
YZM000915-1mg 1mg 99.6% ¥ 1170.00 ¥ 1170.00 2-3天
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¥ 0.00
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中文别名 PF-06380101(1436391-86-4,AUR-0101),PF 06380101,PF06380101, Auristatin 0101
英文别名 PF-06380101(1436391-86-4),PF 06380101,PF06380101, Auristatin 0101,AUR-0101
CAS号 1436391-86-4
SMILES CC[C@H](C)[C@@H]([C@@H](CC(N1[C@@H](CCC1)[C@@H]([C@@H](C)C(N[C@H](C2=NC=CS2)CC3=CC=CC=C3)=O)OC)=O)OC)N(C([C@H](C(C)C)NC(C(C)(C)N)=O)=O)C
Inchi InChI=1S/C39H62N6O6S/c1-11-25(4)33(44(8)37(48)32(24(2)3)43-38(49)39(6,7)40)30(50-9)23-31(46)45-20-15-18-29(45)34(51-10)26(5)35(47)42-28(36-41-19-21-52-36)22-27-16-13-12-14-17-27/h12-14,16-17,19,21,24-26,28-30,32-34H,11,15,18,20,22-23,40H2,1-10H3,(H,42,47)(H,43,49)/t25-,26+,28-,29-,30+,32-,33-,34+/m0/s1
InchiKey QAAFNSMAIAVCHE-BZLYQNAUSA-N
分子式 Formula C39H62N6O6S
分子量 Molecular Weight 743.01
闪点 FP 500.0±34.3 °C
熔点 Melting point No data available
沸点 Boiling point 903.1±65.0 °C at 760 mmHg
Polarizability极化度 81.5±0.5 10-24cm3
密度 Density 1.1±0.1 g/cm3
蒸汽压 Vapor Pressure 0.0±0.3 mmHg at 25°C
溶解度Solubility 生物体外In Vitro:DMSO溶解度≥ 65 mg/mL(87.48 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状 白色至灰白色固体粉末
储藏条件 Storage conditions 在-20°C条件下保存3年,在4°C条件下保存2年

PF-06380101(1436391-86-4,AUR-0101)实验注意事项:
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染

PF-06380101(1436391-86-4,AUR-0101) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tag:PF-06380101(1436391-86-4,AUR-0101),PF-06380101试剂,PF-06380101抑制剂,PF-06380101的纯度,PF-06380101的作用,PF-06380101的效果,PF-06380101应用,PF-06380101的外观,PF-06380101的合成,PF-06380101的溶解度,PF-06380101的生产
产品说明 PF-06380101(1436391-86-4,AUR-0101)是一种微管抑制剂,PF-06380101具有强细胞毒性
IntroductionPF-06380101 (1436391-86-4, AUR-0101) is a microtubule inhibitor, PF-06380101 has strong cytotoxicity
Application1
Application2
Application3
Trop-2, also known as TACSTD2, EGP-1, GA733-1, and M1S1, is frequently expressed on a variety of human carcinomas, and its expression is often associated with poor prognosis of the diseases. However, it is also present on the epithelium of several normal tissues. A comprehensively designed Trop-2-targeting antibody-drug conjugate (ADC), balancing both efficacy and toxicity, is therefore necessary to achieve clinical utility. To this end, we developed a cleavable Trop-2 ADC (RN927C) using a site-specific transglutaminase-mediated conjugation method and a proprietary microtubule inhibitor (MTI) linker-payload, PF-06380101. Robust in vitro cytotoxicity of RN927C was observed on a panel of Trop-2-expressing tumor cell lines, with IC;50; generally in the subnanomolar range. As expected for an MTI-containing ADC, RN927C readily induced mitotic arrest of treated cells in vitro and in vivo, followed by subsequent cell death. The in vivo efficacy of RN927C was tested in multiple cell line and patient-derived xenograft tumor models, including pancreatic, lung, ovarian, and triple-negative breast tumor types. Single-dose administration of RN927C at 0.75 to 3 mg/kg was generally sufficient to induce sustained regression of Trop-2-expressing tumors and showed superior efficacy over standard treatment with paclitaxel or gemcitabine.
1.Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications.
Maderna A;Doroski M;Subramanyam C;Porte A;Leverett CA;Vetelino BC;Chen Z;Risley H;Parris K;Pandit J;Varghese AH;Shanker S;Song C;Sukuru SC;Farley KA;Wagenaar MM;Shapiro MJ;Musto S;Lam MH;Loganzo F;O'Donnell CJ J Med Chem. 2014 Dec 26;57(24):10527-43. doi: 10.1021/jm501649k. Epub 2014 Dec 9.
Auristatins, synthetic analogues of the antineoplastic natural product Dolastatin 10, are ultrapotent cytotoxic microtubule inhibitors that are clinically used as payloads in antibody-drug conjugates (ADCs). The design and synthesis of several new auristatin analogues with N-terminal modifications that include amino acids with α,α-disubstituted carbon atoms are described, including the discovery of our lead auristatin, PF-06380101. This modification of the peptide structure is unprecedented and led to analogues with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs. In addition, auristatin cocrystal structures with tubulin are being presented that allow for the detailed examination of their binding modes. A surprising finding is that all analyzed analogues have a cis-configuration at the Val-Dil amide bond in their functionally relevant tubulin bound state, whereas in solution this bond is exclusively in the trans-configuration. This remarkable observation shines light onto the preferred binding mode of auristatins and serves as a valuable tool for structure-based drug design.
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