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PF-06380101
- names：
PF-06380101
- CAS號：
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(1436391-86-4,AUR-0101)是一種微管抑制劑，PF-06380101具有強(qiáng)細(xì)胞毒性，PF-06380101是新型的細(xì)胞毒性Dolastatin 10類似物,PF-06380101與用于ADC制備的其他合成澳瑞他汀類似物相比，在腫瘤細(xì)胞增殖測定中具有出色的功效，并且具有不同的ADME特性。
| 貨品編碼 | 規(guī)格 | 純度 | 價格 (￥) | 現(xiàn)價(￥) | 特價(￥) | 庫存描述 | 數(shù)量 | 總計(jì) (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000915-5mg | 5mg | 99.6% | ￥ 3543.00 | ￥ 3543.00 | 2-3天 | ￥ 0.00 | ||
| YZM000915-1mg | 1mg | 99.6% | ￥ 1170.00 | ￥ 1170.00 | 2-3天 | ￥ 0.00 |
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| 中文別名 | PF-06380101(1436391-86-4,AUR-0101),PF 06380101,PF06380101, Auristatin 0101 |
| 英文別名 | PF-06380101(1436391-86-4),PF 06380101,PF06380101, Auristatin 0101,AUR-0101 |
| CAS號 | 1436391-86-4 |
| 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 |
| 溶解度Solubility | 生物體外In Vitro:DMSO溶解度≥ 65 mg/mL(87.48 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知. |
| 性狀 | 白色至灰白色固體粉末 |
| 儲藏條件 Storage conditions | 在-20°C條件下保存3年,在4°C條件下保存2年 |
PF-06380101(1436391-86-4,AUR-0101)實(shí)驗(yàn)注意事項(xiàng)：
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡，穿戴防護(hù)服和口罩，佩戴手套，避免與皮膚接觸。
2.實(shí)驗(yàn)過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)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試劑,PF-06380101抑制劑,PF-06380101的純度,PF-06380101的作用,PF-06380101的效果,PF-06380101應(yīng)用,PF-06380101的外觀,PF-06380101的合成,PF-06380101的溶解度,PF-06380101的生產(chǎn)
| 產(chǎn)品說明 | PF-06380101(1436391-86-4,AUR-0101)是一種微管抑制劑，PF-06380101具有強(qiáng)細(xì)胞毒性 |
| Introduction | PF-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.
| 警示圖 | |
| 危險性 | warning |
| 危險性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害 |
| 安全防護(hù) | P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護(hù)理 |
| 備注 | 實(shí)驗(yàn)過程中防止吸入、食入，做好安全防護(hù) |
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.
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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