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[CAS NO. 847871-99-2]  Lenalidomidehemihydrate

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PRODUCTS SPECIFICATIONS [847871-99-2]

Catalog
HY-A0003B
Brand
MCE
CAS
847871-99-2

DESCRIPTION [847871-99-2]

Overview

MDLMFCD28167742
Molecular Weight268.27
Molecular FormulaC13H14N3O3.5
SMILESO=C1N(C2C(NC(CC2)=O)=O)CC3=C(N)C=CC=C31.[0.5 H2O]

For research use only. We do not sell to patients.

26 Publications Citing Use of MCE


Summary

Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN) , and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells [1] [2] .


IC50 & Target

Cereblon


In Vitro

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 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 [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 [5] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

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 [4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT03050450 Johns Hopkins All Children´s Hospital
Central Nervous System Tumors
August 10, 2016 Phase 1
NCT03015792 Mayo Clinic|National Cancer Institute (NCI)
Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma
March 10, 2017 Phase 1|Phase 2
NCT01169298 Celgene
Adult T-cell Leukemia-Lymphoma|Peripheral T-cell Lymphoma
July 1, 2010 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 186.38 mM ; Need ultrasonic)

H 2 O : 0.1 mg/mL ( 0.37 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7276 mL 18.6379 mL 37.2759 mL
5 mM 0.7455 mL 3.7276 mL 7.4552 mL
10 mM 0.3728 mL 1.8638 mL 3.7276 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (9.32 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.32 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.32 mM); Clear solution

* All of the co-solvents are available by MCE.


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