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来那度胺半水合物

Lenalidomide (hemihydrate)

CAS: 847871-99-2

Molecular Formula: C26H28N6O7

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来那度胺半水合物 - Names and Identifiers

Name Lenalidomide (hemihydrate)
Synonyms CC-5013 hemihydrate
LenalidoMide (heMihydrate)
Lenalidomide (hemihydrate)
Lenalidomide hemihydrate (Revlimid, CC 5013)
CAS 847871-99-2

来那度胺半水合物 - Physico-chemical Properties

Molecular FormulaC26H28N6O7
Molar Mass536.53652
Solubility 10 mM in DMSO
Storage Condition-20℃
In vitro study 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. Dose-dependent interaction with the CRBN-DDB1 complex is observed with Thalidomide, Lenalidomide and Pomalidomide, with IC 50 values of ~30 μM, ~3 μM and ~3 μM, respectively, These reduced CRBN expression cells (U266-CRBN 60 and U266-CRBN 75 ) are less responsive than the parental cells to antiproliferative effects Lenalidomide across a dose-response range of 0.01 to 10 μM. 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.
In vivo study The toxicity of Lenalidomide doses up to 15, 22.5, and 45 mg/kg via IV, IP, and PO routes of administration. Limited by solubility in our PBS dosing vehicle, these maximum achievable Lenalidomide doses are well tolerated with the exception of one mouse death (of four total dosed) at the 15 mg/kg IV dose. Notably, no other toxicities are observed in the study at IV doses of 15 mg/kg (n=3) or 10 mg/kg (n=45) or at any other dose level through IV, IP, and PO routes.

来那度胺半水合物 - Preparation solution concentration reference

 1mg5mg10mg
1 mM3.728 ml18.638 ml37.276 ml
5 mM0.746 ml3.728 ml7.455 ml
10 mM0.373 ml1.864 ml3.728 ml
5 mM0.075 ml0.373 ml0.746 ml
Last Update:2024-01-02 23:10:35

来那度胺半水合物 - Reference Information

biological activity lenlidomide hydrate (CC-5013 hemihydrate) is a derivative of alidomide and an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand for the ubiquitin E3 ligase cereblon (CRBN), two lymphatic transcription factors IKZF1 and IKZF3 were selectively ubiquitinated and degraded by CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrate (CC-5013 hemihydrate) specifically inhibits the growth of mature B- cell lymphomas, including multiple myeloma, and induces the release of interleukin-2 from T cells (IL-2).
Last Update:2024-04-10 22:29:15
来那度胺半水合物
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Email: Int06@meryer.com
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View History
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