Lenalidomide|cas 191732-72-6|DC Chemicals

Cas No.:	191732-72-6
Chemical Name:	Lenalidomide
Synonyms:	Lenalidomide;3-(7-amino-3-oxo-1h-isoindol-2-yl)piperidine-2,6-dione;LenalidomideLenalidomide;1-Oxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindoline;3-(4-Amino-1,3-dihydro-1-oxo-2H-isoindol-2-yl)-2,6-piperidinedione;CC-5013;Revlimi;Lenalidomide(other anti-cancers);(3S)-3-(4-Amino-1-oxo-1,3-dihydro-2H-isoindol-2-yl)piperidine-2,6-dione;3-(4-Amino-1-oxo-1,3-dihydro-2H-isoindol-2-yl)piperidine-2,6-dione;3-(4-Amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione;Lenalidomide (CC-5013);Lenalidomide (CC-5013, Revlimid®); Arava;CC5013;Faslodex;Fulvestrant;HWA 486;ICI182780;Leflunomid;Leflunomida;Leflunomide;Leflunomidum;lefunamide;ZD9238;ZM182780;1-Oxo-4-amino-2-(2,6-dioxopiperidin-3-yl)isoindole;3-(4-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione;E3 Ligase ligand;3-(4-Amino-1-oxoisoindolin-2-yl)piperidin-2,6-dione;Revlimid;To the amine;LenalidoMide-d5;LenalidoMide (RevliMid);CC 5013;Lenalidomide ,98%;SGT67 lila@tuskwei.com;Revimid;IMiD3;CDC 501;Revlimid (lenalidomide);2,6-Piperidinedione, 3-(4-amino-1,3-dihydro-1-oxo-2H-isoindol-2-yl)-;Revlimid (TN);3-(4-amino-1-oxo-2,3-dihydro-1H-isoindol-2-yl)piperidine-2,6-dione;DSSTox_RID_
SMILES:	O=C1C2C([H])=C([H])C([H])=C(C=2C([H])([H])N1C1([H])C(N([H])C(C([H])([H])C1([H])[H])=O)=O)N([H])[H]
Formula:	C₁₃H₁₃N₃O₃
M.Wt:	259.2606
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Lenalidomide is a potent inhibitor of TNF-α used as a immunomodulatory drug. It has also been shown to have anti-angiogenic properties.
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].
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 IC50 values of ~30 μM, ~3 μM and ~3 μM, respectively, These reduced CRBN expression cells (U266-CRBN60 and U266-CRBN75) 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].

Cat. No.	Product name	Field of application
DC60864	D927 (DS11252927)	D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers blood glucose concentrations.
DC60863	D223 (DS02312223)	D223 is a molecular glue and promotes glucose uptake in the absence of insulin. D223 also increases the affinity of RAS binding to PI3Kα by ~500-fold.
DC60858	LC-04-045	LC-04-045 is a leading NEK7 molecular glue degrader with DC50 of 7 nM and Dmax of 90 % in MOLT-4 cells. LC-04-045 displays high selectivity for NEK7 across the proteome.
DC60852	PVTX-405	PVTX-405 is a potent, effective, highly selective, and orally efficacious IKZF2 molecular glue degrader with DC50 of 0.7 nM. PVTX-405 in combination with anti-PD1 or anti-LAG3 significantly increases animal survival compared to anti-PD1 or anti-LAG3 alone.
DC60837	MGD-28	MGD-28 is a potent molecular glue degrader that demonstrates significant in vitro efficacy against various hematological cancer cell lines. It induces degradation of Ikaros family zinc finger proteins 1, 2, and 3 (IKZF1/2/3) and casein kinase 1 alpha (CK1α) with nanomolar potency via a Cullin-cereblon (CRBN) dependent pathway. Compared to lenalidomide and pomalidomide, MGD-28 achieves deeper, faster, and more potent degradation of these neosubstrates. Additionally, MGD-28 exhibits broad antiproliferative activity in multiple solid malignancies and shows preferential cytotoxicity toward multiple myeloma patient-derived cells at various disease stages.
DC67413	MRT-23227
DC67412	MRT-3486	MRT-3486 (Compound 5) is a cereblon-based NEK7 molecular glue degrader. MRT-3486 can be used for autoinflammatory diseases research.
DC67411	MRT-7612
DC67410	MRT-10350
DC67407	IKZF1-degrader-1	IKZF1-degrader-1 (Compound 9-B) is a highly potent molecular glue that achieves sub-nanomolar degradation of IKZF1 (DC50 = 0.134 nM), demonstrating significant therapeutic potential for targeting IKZF1-dependent malignancies.