| Identification | Back Directory | [Name]
CC 5013 hydrochloride | [CAS]
1243329-97-6 | [Synonyms]
Lenalidomide HCl
CC5013 hydrochloride
CC-5013 hydrochloride
CC 5013 hydrochloride
RevliMid hydrochloride
LenalidoMide (hydrochloride) | [Molecular Formula]
C13H14ClN3O3 | [MDL Number]
MFCD26960943 | [MOL File]
1243329-97-6.mol | [Molecular Weight]
295.72 |
| Hazard Information | Back Directory | [Biological Activity]
lenalidomideis a derivative of thalidomide introduced in 2004. lenalidomide (revlimid, cc-5013) is a tnf-α secretion inhibitor with ic50 of 13 nm. | [in vitro]
lenalidomide strongly induces il-2 and sil-2r production. lenalidomide-induced tyrosine phosphorylation of cd28 on t cells is followed by a down-stream activation of nf-κb [2]. lenalidomide and pomalidomide inhibits autoubiquitination of crbn in hek293 t cells expressing thalidomide-binding competent wild-type crbn, but not thalidomide-binding defective crbn (yw/aa). overexpression of crbn wild-type protein, but not crbn (yw/aa) mutant protein, in kms12 myeloma cells, amplifies pomalidomide-mediated reductions in c-myc and irf4 expression and increases in p21(waf-1) expression. long-term selection for lenalidomide resistance in h929 myeloma cell lines is accompanied by a reduction in crbn, while in df15r myeloma cells resistant to both pomalidomide and lenalidomide, crbn protein is undetectable [3]. | [in vivo]
pharmacokinetic studies evaluated doses of 0.5, 1.5, 5, and 10 mg/kg iv and 0.5 and 10 mg/kg doses for ip and oral routes. liquid chromatography-tandem mass spectrometry was used to quantify lenalidomide in plasma, brain, lung, liver, heart, kidney, spleen, and muscle [4]. treatment with either thalidomide or lenalidomide attenuated weight loss, enhanced motor performance, decreased motor neuron cell death, and significantly increased the life span in g93a transgenic mice [5]. | [IC 50]
value: 13 nm [1] lenalidomideis a derivative of thalidomide introduced in 2004. lenalidomide (revlimid, cc-5013) is a tnf-α secretion inhibitor with ic50 of 13 nm. in vitro: lenalidomide strongly induces il-2 and sil-2r production. lenalidomide-induced tyrosine phosphorylation of cd28 on t cells is followed by a down-stream activation of nf-κb [2]. lenalidomide and pomalidomide inhibits autoubiquitination of crbn in hek293 t cells expressing thalidomide-binding competent wild-type crbn, but not thalidomide-binding defective crbn (yw/aa). overexpression of crbn wild-type protein, but not crbn (yw/aa) mutant protein, in kms12 myeloma cells, amplifies pomalidomide-mediated reductions in c-myc and irf4 expression and increases in p21(waf-1) expression. long-term selection for lenalidomide resistance in h929 myeloma cell lines is accompanied by a reduction in crbn, while in df15r myeloma cells resistant to both pomalidomide and lenalidomide, crbn protein is undetectable [3]. in vivo: pharmacokinetic studies evaluated doses of 0.5, 1.5, 5, and 10 mg/kg iv and 0.5 and 10 mg/kg doses for ip and oral routes. liquid chromatography-tandem mass spectrometry was used to quantify lenalidomide in plasma, brain, lung, liver, heart, kidney, spleen, and muscle [4]. treatment with either thalidomide or lenalidomide attenuated weight loss, enhanced motor performance, decreased motor neuron cell death, and significantly increased the life span in g93a transgenic mice [5]. toxicity: international staging system iii received a combination therapy of lenalidomide (15 mg, day 1 - 21) with dexamethasone (40 mg, day 1, 8, 15, 22). after 4 days on chemotherapy, he experienced worsened dyspnea and was urgently hospitalized because of acute respiratory failure [6]. |
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