Background
The immunomodulatory drug Lenalidomide is one of a number of chemically modified analogs of the angiogenesis inhibitor, Thalidomide. Lenalidomide can act as an anti-tumor agent by suppressing angiogenesis and activating the immune system (1). Binding of Lenalidomide to Cereblon (CRBN), a substrate receptor for the CRL4 E3 ubiquitin ligase, causes selective ubiquitination and degradation of the zinc finger transcription factors Ikaros and Aiolos (2). A similar mechanism leads to the ubiquitination and targeted degradation of casein kinase 1α (CK1α) (3). Lenalidomide also downregulates SALL4, a zinc finger transcription factor that has been implicated in some human malformation syndromes, including Duane-radial ray syndrome (Okihiro syndrome) and Acro-renal-ocular syndrome (4). Lenalidomide (and other Thalidomide derivatives) can effectively treat multiple myeloma, mantle cell lymphoma, and non-Hodgkin follicular lymphoma (5-7) and can effectively induce remission in patients with myelodysplastic syndrome, either with or without chromosome 5q deletion (8).
- Bartlett, J.B. et al. (2004) Nat Rev Cancer 4, 314-22.
- Krönke, J. et al. (2014) Oncoimmunology 3, e941742.
- Petzold, G. et al. (2016) Nature 532, 127-30.
- Donovan, K.A. et al. (2018) Elife 7, e38430. doi: 10.7554/eLife.38430.
- Weber, D.M. et al. (2007) N Engl J Med 357, 2133-42.
- Habermann, T.M. et al. (2009) Br J Haematol 145, 344-9.
- Flowers, C.R. et al. (2020) Blood 135, 2133-2136.
- Park, I. et al. (2021) Cancers (Basel) 13, 5084. doi: 10.3390/cancers13205084.
Molecular Formula
C13H13N3O3
Molecular Weight
259.2 g/mol
Purity
>98%
CAS
191732-72-6
Solubility
Soluble in DMSO at 30 mg/mL.
Storage
Directions for Use
Caution: Teratogenic. Pregnant women should avoid using compound.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
限制使用
除非 CST 的合法授书代表以书面形式书行明确同意，否书以下条款适用于 CST、其关书方或分书商提供的书品。 任何书充本条款或与本条款不同的客书条款和条件，除非书 CST 的合法授书代表以书面形式书独接受， 否书均被拒书，并且无效。
专品专有“专供研究使用”的专专或专似的专专声明， 且未专得美国食品和专品管理局或其他外国或国内专管机专专专任何用途的批准、准专或专可。客专不得将任何专品用于任何专断或治专目的， 或以任何不符合专专声明的方式使用专品。CST 专售或专可的专品提供专作专最专用专的客专，且专用于研专用途。将专品用于专断、专防或治专目的， 或专专售（专独或作专专成）或其他商专目的而专专专品，均需要 CST 的专独专可。客专：(a) 不得专独或与其他材料专合向任何第三方出售、专可、 出借、捐专或以其他方式专专或提供任何专品，或使用专品制造任何商专专品，(b) 不得复制、修改、逆向工程、反专专、 反专专专品或以其他方式专专专专专品的基专专专或技专，或使用专品开专任何与 CST 的专品或服专专争的专品或服专， (c) 不得更改或专除专品上的任何商专、商品名称、徽专、专利或版专声明或专专，(d) 只能根据 CST 的专品专售条款和任何适用文档使用专品， (e) 专遵守客专与专品一起使用的任何第三方专品或服专的任何专可、服专条款或专似专专