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PROTAK™ Lenalidomide hydrochloride
$180/ 50mg
Specification
QuantityTotal: $180
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Product Information
CAS No.1243329-97-6
Name3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione hydrochloride
Purity>98.00%
FormulaC13H14ClN3O3
M.W.295.72
Solubility≥72.2 mg/mL in DMSO, <1.5 mg/mL in H2O, ≥1.83 mg/mL in EtOH
Storage/StabilityStore at -20°C
BackgroundLenalidomide hydrochloride interacts with E3 ligase cereblon, links casein kinase 1A1 (CKIα) to the human E3 ligase cereblon, and induces CKIa degradation.
Lenalidomide is potent in stimulating T cell proliferation and IFN-γ and IL-2 production. Lenalidomide has been shown to inhibit production of pro inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 and elevate the production of anti-inflammatory cytokine IL-10 from human PBMCs. Lenalidomide downregulates the production of IL-6 directly and also by inhibiting multiple myeloma (MM) cells and bone marrow stromal cells (BMSC) interaction, which augments the apoptosis of myeloma cells[2]. Dose-dependent interaction with the CRBN-DDB1 complex is observed with Thalidomide, Lenalidomide and Pomalidomide, with IC50 values of ~30 μM, ~3 μM and ~3 μM, respectively, These reduced CRBN expression cells (U266-CRBN60 and U266-CRBN75) are less responsive than the parental cells to antiproliferative effects Lenalidomide across a dose-response range of 0.01 to 10 μM[3]. Lenalidomide, a thalidomide analog, functions as a molecular glue between the human E3 ubiquitin ligase cereblon and CKIα is shown to induce the ubiquitination and degradation of this kinase, thus presumably killing leukemic cells by p53 activation.
Lenalidomide is potent in stimulating T cell proliferation and IFN-γ and IL-2 production. Lenalidomide has been shown to inhibit production of pro inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 and elevate the production of anti-inflammatory cytokine IL-10 from human PBMCs. Lenalidomide downregulates the production of IL-6 directly and also by inhibiting multiple myeloma (MM) cells and bone marrow stromal cells (BMSC) interaction, which augments the apoptosis of myeloma cells[2]. Dose-dependent interaction with the CRBN-DDB1 complex is observed with Thalidomide, Lenalidomide and Pomalidomide, with IC50 values of ~30 μM, ~3 μM and ~3 μM, respectively, These reduced CRBN expression cells (U266-CRBN60 and U266-CRBN75) are less responsive than the parental cells to antiproliferative effects Lenalidomide across a dose-response range of 0.01 to 10 μM[3]. Lenalidomide, a thalidomide analog, functions as a molecular glue between the human E3 ubiquitin ligase cereblon and CKIα is shown to induce the ubiquitination and degradation of this kinase, thus presumably killing leukemic cells by p53 activation.
Price180$
≥72.2 mg/mL in DMSO, <1.5 mg/mL in H2O, ≥1.83 Store at -20°C Lenalidomide hydrochloride interacts with E3 ligase kinase 1A1 (CKIα) to the human E3 ligase cereblon, degradation.
E31P14015-1, E31P14015-2 PROTAK™ Lenalidomide hydrochloride 50mg,100mg 1243329-97-6 3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione
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