d***e
发帖数: 1215 | 1 Hydrazone linker其实没有那么不稳定，但是这么说的人太多了，弄成了主流理论了。
Mylotarg不稳定的主要原因是drug load distribution不好，现在有几个在临床的ADC
同样用的是hydrazone linker,但是各种指标都还不算差。
lysine |
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b****u
发帖数: 2771 | 2 贵公司是P 家吧,
那三期的trial 还舍不得扔，FDA都hold不住了。
稳定性是相对的，这几代ADC 这hydrazone liner是最不稳定的，应该是公认的吧
mylotarg之后 的hydrazone linker ADC基本都是降低dosage,
毒性小了， 药效也不显著了。 还是早死早超生的好
ADC |
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b****u
发帖数: 2771 | 3 贵公司是P 家吧,
那三期的trial 还舍不得扔，FDA都hold不住了。
稳定性是相对的，这几代ADC 这hydrazone liner是最不稳定的，应该是公认的吧
mylotarg之后 的hydrazone linker ADC基本都是降低dosage,
毒性小了， 药效也不显著了。 还是早死早超生的好
ADC |
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j*********5
发帖数: 6221 | 4 【 以下文字转载自 Chemistry 讨论区 】
发信人: jameslee435 (济南秦琼), 信区: Chemistry
标 题: 转让四面体审稿一篇
发信站: BBS 未名空间站 (Tue Aug 13 13:12:23 2013, 美东)
有需要的PM，收取辛苦费两个包子
Title: An investigation of the deprotonation of hydrazone-based receptors on
interaction with anion: develop a system distinguishing cyanide from anions
signaled by the color |
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g*u
发帖数: 190 | 5 anyone are interested in the following review from "Indian Journal of
Pharmaceutical Sciences".
Keywords: Characterization & Thermal Studies; Cr(III) Mn(III) Fe(III) VO(IV)
Zr(IV) UO2(VI) Complexes; Schiff Base; Isonicotinoyl Hydrazone
Please let me know your name, email and institution.
Thanks, |
|
s**********r
发帖数: 67 | 6 1.Nina G. DOlinnaya, Marta Blumenfeld*, Irena N. Merenkova,etc.,
Oligonucleotide circularization by template-directed chemical ligation, Nucl
. Acids Res. (1993) 21 (23): 5403-5407. doi: 10.1093/nar/21.23.5403
2. Franziska Diezmann, Hendrik Eberhard, Oliver Seitz, Native chemical
ligation in the synthesis of internally modified oligonucleotide–peptide
conjugates, Biopolymers (Pept Sci) 94: 397–404, 2010.
3. K. Achilles, G.v. Kiedrowski,Kinetic model studies on the chemical
ligation of oligonucle... 阅读全帖 |
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s******e
发帖数: 111 | 7 Journal of scientific & industrial research.
44(12), 635-674 Dec 1985
Title: COORDINATION CHEMISTRY OF ACYL, AROYL, HETEROAROYL HYDRAZONES AND
RELATED LIGANDS
Author: DUTTA, RL
please send it to: j******[email protected],
thank you very much! |
|
s******e
发帖数: 111 | 8 Journal of scientific & industrial research.
44(12), 635-674 Dec 1985
Title: COORDINATION CHEMISTRY OF ACYL, AROYL, HETEROAROYL HYDRAZONES AND
RELATED LIGANDS
Author: DUTTA, RL
please send it to: j******[email protected],
thank you very much! |
|
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j*********5
发帖数: 6221 | 9 有需要的PM，收取辛苦费两个包子
Title: An investigation of the deprotonation of hydrazone-based receptors on
interaction with anion: develop a system distinguishing cyanide from anions
signaled by the color |
|
d***e
发帖数: 1215 | 10 是没有那么稳定，但也还真没有“公认”的那么差，至少我知道的几个project各种指
标都还好好的。所谓“毒性小了，药效不显著了”那得看你用什么payload是什么样的
cancer。Seagen的那些payloads虽然没用hydrazone linker, 但是还倒还真是毒性不够
，对好些tumor不work. |
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g**a
发帖数: 953 | 11 求教懂行的大牛们这种方法靠谱吗? Albumin-emch-doxorubicin
遇到肿瘤周围的酸性环境就释放阿霉素？先谢谢了
Aldoxorubicin (formlerly INNO-206) is a tumor-targeted doxorubicin conjugate
. Specifically, it is the (6-Maleimidocaproyl) hydrazone of doxorubicin.
Essentially, this chemical name describes doxorubicin (DOXO) attached to an
acid sensitive linker (EMCH). We believe this novel agent has attributes
that improve on native doxorubicin including reduction of adverse events,
improvement in efficacy and the ability to reach the tumor mor... 阅读全帖 |
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