Lenalidomide

Size	Price	Stock	Quantity
25 g	$298	In stock

Purity

≥98% (HPLC)

Solubility

DMSO:25.93mg/mL

Appearance

White solid powder

ShelfLife

>2 years if stored properly

Storage

Store at -20°C

Shipping

Room temperature in continental US; may vary elsewhere.

Synonyms

CC5013; CC-5013; CC 5013; IMiD1; Lenalidomide; US brand name: Revlimid

Melting Point

>250°C (dec.)

Chemical Name

3-(4-Amino-1,3-dihydro-1-oxo-2H-isoindol-2-yl)-2,6-piperidinedione

InChI Key

InChI=1S/C13H13N3O3/c14-9-3-1-2-7-8(9)6-16(13(7)19)10-4-5-11(17)15-12(10)18/h1-3,10H,4-6,14H2,(H,15,17,18)

InChI

GOTYRUGSSMKFNF-UHFFFAOYSA-N

Canonical SMILES

NC1=C2CN(C(C2=CC=C1)=O)C3CCC(NC3=O)=O

Biological Activity

Thalidomide analog. Immune modulatory drug and cereblon binding compound. Induces ubiquitination and degradation of casein kinase (CK) 1α by the E3 ubiquitin ligase CRL4CRBN. Also TNF-α inhibitor and angiogenesis inhibitor. Promotes degradation of transcription factor SALL4.

1.Oral Ixazomib, Lenalidomide, and Dexamethasone for Multiple Myeloma.

Moreau P, Masszi T, Grzasko N, Bahlis NJ, Hansson M, Pour L, Sandhu I, Ganly P, Baker BW, Jackson SR, Stoppa AM, Simpson DR, Gimsing P, Palumbo A, Garderet L, Cavo M, Kumar S, Touzeau C, Buadi FK, Laubach JP, Berg DT, Lin J, Di Bacco A, Hui AM, van de Vel N Engl J Med. 2016 Apr 28;374(17):1621-34. doi: 10.1056/NEJMoa1516282.

BACKGROUND: Ixazomib is an oral proteasome inhibitor that is currently being studied for the treatment of multiple myeloma.

2.A study of high-dose lenalidomide induction and low-dose lenalidomide maintenance therapy for patients with hypomethylating agent refractory myelodysplastic syndrome.

Cherian MA1, Tibes R2, Gao F3, Fletcher T1, Fiala M1, Uy GL1, Westervelt P1, Jacoby MA1, Cashen AF1, Stockerl-Goldstein K1, DiPersio JF1, Vij R1. Leuk Lymphoma. 2016 Apr 27:1-6. [Epub ahead of print]

Myelodysplastic syndromes (MDS) are clonal hematopoietic disorders characterized by bone marrow failure which frequently progress to acute myeloid leukemia. Patients who fail to respond to, or progress on first-line DNA hypomethylating agents (HMA) have a poor prognosis. Conventionally dosed lenalidomide has activity in 5q-MDS. In other subtypes, it may reduce RBC transfusion requirements but does not result in cytogenetic responses. We previously reported that high-dose lenalidomide induction (50 mg/day) results in complete remissions in a high fraction of patients. We, therefore, conducted a Phase 2 trial of the same regimen in MDS refractory to HMA. Marrow complete remissions were seen in 33% of patients and hematological improvement in 8% of patients. Significant infections complicated more than 50% of cases. Future trials to explore alternative dosing schedules of high-dose lenalidomide to increase efficacy while decreasing toxicity are warranted.

HPLC

HNMR

Hi, how does Lenalidomide exert anti-cancer effects?

Lenalidomide triggers the activation of pro-apoptotic caspase-8, enhances tumor cell sensitivity to FAS-induced apoptosis, and downregulates NF-κB, an anti-apoptotic protein.7 Independent of its immunomodulatory effects, lenalidomide mediates anti-angiogenic effects by inhibiting angiogenic growth factors released by tumor cells, such as vascular endothelial growth factor (VEGF), basic fibroblastic-growth factor (BFGF), and hepatocyte-growth factor.

15/12/2017

Dear Sirs, how does Lenalidomide augment the apoptosis of myeloma cells?

Hello, 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.

15/4/2018

Would you like to tell me the toxicity of Lenalidomide?

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.

31/5/2018

block cell adhesion molecules

In vitro, lenalidomide blocks cell adhesion molecules such as ICAM-1, LFA-1, β2 and β3 integrins, as well as gap-junction function, thereby preventing metastasis of malignant cells. I'm glad to have such a good product.

26/11/2016

inhibit growth of mature B-cell lymphomas

We used this in cell culture studies and got good results. Lenalidomide specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.

28/11/2016

stimulate T cell proliferation

I think it's not bad! Lenalidomide is potent in stimulating T cell proliferation and IFN-γ and IL-2 production.

21/2/2021

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* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂