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
- Molecular Weight:
- 536.53652
- MDL Number:
- MFCD28167742
- MOL File:
- 847871-99-2.mol
storage temp. | Store at -20°C |
---|---|
solubility | DMSO : 50 mg/mL (186.38 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) |
form | Powder |
color | Off-white to pink |
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 |
FDA UNII | XQT0NAW8WD |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
---|---|
Signal word | Warning |
Hazard statements | H302-H315-H319-H335 |
Precautionary statements | P261-P305+P351+P338 |
LenalidoMide (heMihydrate) price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ApexBio Technology | B1188 | Lenalidomidehemihydrate | 847871-99-2 | 50mg | $113 | 2021-12-16 | Buy |
ApexBio Technology | B1188 | Lenalidomidehemihydrate | 847871-99-2 | 100mg | $180 | 2021-12-16 | Buy |
ApexBio Technology | B1188 | Lenalidomidehemihydrate | 847871-99-2 | 500mg | $300 | 2021-12-16 | Buy |
ApexBio Technology | B1188 | Lenalidomidehemihydrate | 847871-99-2 | 1g | $465 | 2021-12-16 | Buy |
Crysdot | CD31000637 | Lenalidomidehemihydrate 98+% | 847871-99-2 | 50mg | $53 | 2021-12-16 | Buy |
LenalidoMide (heMihydrate) Chemical Properties,Uses,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
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LenalidoMide (heMihydrate) Preparation Products And Raw materials
Raw materials
Preparation Products
LenalidoMide (heMihydrate) Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
SHANDONG BOYUAN PHARMACEUTICAL CO., LTD. | +86-0531-69954981 +8615666777973 | dwyane.wang@boyuanpharm.com | China | 211 | 58 |
Jinan Honest Pharm Co., Ltd | +8615318812076 | zpy8217@163.com | China | 286 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
CR Corporation Lomited | fred.wen@crcorporation.cn | CHINA | 12069 | 58 | |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
Jilin Chinese Academy of Sciences-yanshen Technology | +undefined18143011203 | info@chemextension.com | China | 42057 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
Hunan Hui Bai Shi Biotechnology Co., Ltd. | 0731-85526065 13308475853 | ivy@hnhbsj.com | China | 4550 | 62 |
Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7553 | 61 |