LenalidoMide (heMihydrate) Struktur

LenalidoMide (heMihydrate)

Bezeichnung:LenalidoMide (heMihydrate)

CAS-Nr847871-99-2

Englisch Name:LenalidoMide (heMihydrate)

CBNumberCB22682011

SummenformelC26H28N6O7

Molgewicht536.53652

MOL-Datei847871-99-2.mol

LenalidoMide (heMihydrate) physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	DMSO : 50 mg/mL (186.38 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
Aggregatzustand	Powder
Farbe	Off-white to pink
InChI	InChI=1S/2C13H13N3O3.H2O/c214-9-3-1-2-7-8(9)6-16(13(7)19)10-4-5-11(17)15-12(10)18;/h21-3,10H,4-6,14H2,(H,15,17,18);1H2
InChIKey	OTJHSDXKMBRCMM-UHFFFAOYSA-N

Gefahreninformationscode (GHS)

LenalidoMide (heMihydrate) Chemische Eigenschaften,Einsatz,Produktion Methoden

Biologische Aktivität
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

LenalidoMide (heMihydrate) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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