1243329-97-6 Usage
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].
Check Digit Verification of cas no
The CAS Registry Mumber 1243329-97-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,4,3,3,2 and 9 respectively; the second part has 2 digits, 9 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1243329-97:
(9*1)+(8*2)+(7*4)+(6*3)+(5*3)+(4*2)+(3*9)+(2*9)+(1*7)=146
146 % 10 = 6
So 1243329-97-6 is a valid CAS Registry Number.
1243329-97-6Relevant articles and documents
ACID ADDITION SALTS OF LENALIDOMIDE
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, (2011/05/11)
The invention relates to acid addition salts of lenalidomide as well as to desirable polymorphic forms of lenalidomide hydrogen sulfate. Furthermore, the invention provides a process for producing acid addition salts of lenalidomide, which optionally can comprise a further step producing lenalidomide in form of the free base.
