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2149584-00-7
  • names:

    Ala-Ala-Asn-PAB

  • CAS號(hào):

    2149584-00-7

    MDL Number: MFCD28898921
  • MF(分子式): C17H25N5O5 MW(分子量): 379.41
  • EINECS: Reaxys Number:
  • Pubchem ID:118966102 Brand:BIOFOUNT
Ala-Ala-Asn-PAB
Ala-Ala-Asn-PAB(2149584-00-7)是抗體偶聯(lián)藥物 (ADCs) 的常用一種蛋白可降解 (cleavable) 的 ADC linker。
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中文別名 Ala-Ala-Asn-PAB(2149584-00-7);
英文別名 Ala-Ala-Asn-PAB(2149584-00-7);SCHEMBL17615149;HY-129360;CS-0105007;
CAS號(hào) 2149584-00-7
Inchi InChI=1S/C17H25N5O5/c1-9(18)15(25)20-10(2)16(26)22-13(7-14(19)24)17(27)21-12-5-3-11(8-23)4-6-12/h3-6,9-10,13,23H,7-8,18H2,1-2H3,(H2,19,24)(H,20,25)(H,21,27)(H,22,26)/t9-,10-,13-/m0/s1
InchiKey VPXFRPRRAXTBSH-KWBADKCTSA-N
分子式 Formula C17H25N5O5
分子量 Molecular Weight 379.41
溶解度Solubility
性狀 Solid
儲(chǔ)藏條件 Storage conditions 請(qǐng)根據(jù)產(chǎn)品建議的存儲(chǔ)條件進(jìn)行存儲(chǔ),Please store the product under the recommended condition sin the description.

Ala-Ala-Asn-PAB(2149584-00-7)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(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)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(chǔ),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.

Tags:2149584-00-7試劑,2149584-00-7雜質(zhì),2149584-00-7合成,2149584-00-7密度,2149584-00-7旋光度,2149584-00-7溶解度,2149584-00-7閃點(diǎn),2149584-00-7購買,
產(chǎn)品說明 Ala-Ala-Asn-PAB(2149584-00-7)實(shí)驗(yàn)注是抗體偶聯(lián)藥物 (ADCs) 的常用一種蛋白可降解的ADC連接橋
IntroductionAla-Ala-Asn-PAB(2149584-00-7)實(shí)驗(yàn)注s a peptide cleavableADC linkerfor antibodyrug conjugates (ADCs).
Application1
Application2
Application3
Ala-Ala-Asn-PAB(2149584-00-7)藥理學(xué):
Ala-Ala-Asn-PAB(2149584-00-7)是抗體偶聯(lián)藥物 (ADCs) 的常用一種蛋白可降解 (cleavable) 的 ADC linker。
Cheng X, et al. MORAb-202, an Antibody-Drug Conjugate Utilizing Humanized Anti-human FRα Farletuzumab and the Microtubule-targeting Agent Eribulin, has Potent Antitumor Activity. Mol Cancer Ther. 2018
Ala-Ala-Asn-PAB(2149584-00-7)參考文獻(xiàn):
1、MORAb-202, an Antibody-Drug Conjugate Utilizing Humanized Anti-human FRα
Farletuzumab and the Microtubule-targeting Agent Eribulin, has Potent Antitumor Activity Xin Cheng 1, Jing Li 2, Keigo Tanaka 3, Utpal Majumder 4, Andrew Z Milinichik 1, Arielle C Verdi 1, Christopher J Maddage 5, Katherine A Rybinski 5, Shawn Fernando 6, Danielle Fernando 6, Megan Kuc 6, Keiji Furuuchi 5, Frank Fang 2, Toshimitsu Uenaka 5, Luigi Grasso 7, Earl F Albone 8

Abstract Microtubule-targeting agents (MTA) have been investigated for many years as payloads for antibody-drug conjugates (ADC). In many cases, these ADCs have shown limited benefits due to lack of efficacy or significant toxicity, which has spurred continued investigation into novel MTA payloads for next-generation ADCs. In this study, we have developed ADCs using the MTA eribulin, a derivative of the macrocyclic polyether natural product halichondrin B, as a payload. Eribulin ADCs demonstrated in vitro potency and specificity using various linkers and two different conjugation approaches. MORAb-202 is an investigational agent that consists of the humanized anti-human folate receptor alpha (FRA) antibody farletuzumab conjugated via reduced interchain disulfide bonds to maleimido-PEG2-valine-citrulline-p-aminobenzylcarbamyl-eribulin at a drug-to-antibody ratio of 4.0. MORAb-202 displayed preferable biophysical properties and broad potency across a number of FRA-positive tumor cell lines as well as demonstrated improved specificity in vitro compared with farletuzumab conjugated with a number of other MTA payloads, including MMAE, MMAF, and the reducible maytansine linker-payload sulfo-SPDB-DM4. A single-dose administration of MORAb-202 in FRA-positive human tumor cell line xenograft and patient-derived tumor xenograft models elicited a robust and durable antitumor response. These data support further investigation of MORAb-202 as a potential new treatment modality for FRA-positive cancers, using the novel MTA eribulin as a payload.
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