LenalidoMide (heMihydrate)
- Product Name
- LenalidoMide (heMihydrate)
- CAS No.
- 847871-99-2
- Chemical Name
- LenalidoMide (heMihydrate)
- Synonyms
- Lenalidonmide;CC-5013 hemihydrate;LenalidoMide (heMihydrate);Lenalidomide hemihydrate (Revlimid, CC 5013);3-(4-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione hemihydrate;IKZF3,inhibit,IKZF1,ligand,Inhibitor,CC-5013 hemihydrate,degradation,myeloma,Ligands for E3 Ligase,analog,multiple,Lenalidomide hemihydrate,immunomodulatory,E3 ligase-recruiting Moiety,CRL4,ligase,Molecular Glues,cereblon,Apoptosis
- CBNumber
- CB22682011
- Molecular Formula
- C26H28N6O7
- Formula Weight
- 536.53652
- MOL File
- 847871-99-2.mol
LenalidoMide (heMihydrate) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (186.38 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
- form
- Powder
- InChI
- InChI=1S/2C13H13N3O3.H2O/c2*14-9-3-1-2-7-8(9)6-16(13(7)19)10-4-5-11(17)15-12(10)18;/h2*1-3,10H,4-6,14H2,(H,15,17,18);1H2
- InChIKey
- OTJHSDXKMBRCMM-UHFFFAOYSA-N
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- B1188
- Product name
- Lenalidomidehemihydrate
- Packaging
- 50mg
- Price
- $113
- Updated
- 2021/12/16
- Product number
- B1188
- Product name
- Lenalidomidehemihydrate
- Packaging
- 100mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- B1188
- Product name
- Lenalidomidehemihydrate
- Packaging
- 500mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- B1188
- Product name
- Lenalidomidehemihydrate
- Packaging
- 1g
- Price
- $465
- Updated
- 2021/12/16
- Product number
- CD31000637
- Product name
- Lenalidomidehemihydrate
- Purity
- 98+%
- Packaging
- 50mg
- Price
- $53
- Updated
- 2021/12/16
LenalidoMide (heMihydrate) Chemical Properties,Usage,Production
Biological Activity
LenalidoMide (heMihydrate) is a derivative of Thalidomide and an orally active immunomodulator. It is a ligand for the ubiquitin E3 ligase cereblon (CRBN), selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. It specifically inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and induces the release of interleukin-2 (IL-2) from T cells.
in vitro
LenalidoMide (heMihydrate) is potent in stimulating T cell proliferation and IFN-γ and IL-2 production. It 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. It 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 ubiq uitin 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
The toxicity of LenalidoMide (heMihydrate) 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.
target
| Cereblon
|