SML2942

LY2857785 free base

≥98% (HPLC)

• Synonim(y): LY 2857785 free base, LY-2857785 free base, N1-[4-(3-isopropyl-2-methyl-indazol-5-yl) pyrimidin-2-yl]-N4-tetrahydropyran-4-yl-cyclohexane-trans-1, 4-diamine
• Wzór empiryczny (zapis Hilla): C₂₆H₃₆N₆O
• Numer CAS: 1619903-54-6
• Masa cząsteczkowa: 448.60
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD28167812
• Assay: ≥98% (HPLC)
• Form: powder

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C
• SMILES string: CN1C(C(C)C)=C2C(C=CC(C3=NC(N[C@H]4CC[C@H](NC5CCOCC5)CC4)=NC=C3)=C2)=N1
• InChI: 1S/C26H36N6O/c1-17(2)25-22-16-18(4-9-24(22)31-32(25)3)23-10-13-27-26(30-23)29-20-7-5-19(6-8-20)28-21-11-14-33-15-12-21/h4,9-10,13,16-17,19-21,28H,5-8,11-12,14-15H2,1-3H3,(H,27,29,30)/t19-,20-
• InChI key: LHIUZPIDLZYPRL-MXVIHJGJSA-N

Opis

Biochem/physiol Actions

ATP-competitive, potent and reversible CDK9/4/8, DYRK2, FLT3-D835Y inhibitor with anticancer efficacy in vitro and in vivo.

LY2857785 is an ATP-competitive, potent and reversible CDK9/4/8 (IC50 =11 nM/CDK9-CycT, 12 nM/CDK4-CycD1, 16 nM/CDK8-CycC), DYRK2 (IC50 = 44 nM) and FLT3-D835Y (IC50 = 23 nM) inhibitor that significantly reduces cellular RNAP II CTD phosphorylation (U2OS pSer2/pSer5 IC50 =89/42 nM) with good selectivity over a panel of 109 kinase constructs (IC50 = 0.1-1μM/wt FLT3, CDK1/2/3/5/7, PIM1/2; >1 μM/100 kinases). LY2857785 exhibits antiproliferation efficacy in a wide-range cancer cultures (IC50 ∼30 nM-1 μM), and causes AML MV-4-11 xenograft tumor regression in rats (3-9 mg/kg, i.v. infusion Q5Dx5) and mice (8-10 mg/kg, i.v. bolus Q3Dx5) in vivo.

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• WGK: WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable