LY2857785 free base
SIGMA/SML2942 - ≥98% (HPLC)
Synonym: LY 2857785 free base; LY-2857785 free base; N1-
CAS Number: 1619903-54-6
Empirical Formula (Hill Notation): C26H36N6O
Molecular Weight: 448.60
MDL Number: MFCD28167812
Linear Formula: C26H36N6O
Product Type: Chemical
assay | ≥98% (HPLC) |
color | white to beige |
form | powder |
Quality Level | 100 ![]() |
SMILES string | CN1C(C(C)C)=C2C(C=CC(C3=N |
solubility | DMSO: 2 mg/mL, clear |
storage temp. | −20°C |
Biochem/physiol Actions: | 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. |
WGK Germany | WGK 3 |
Flash Point(F) | Not applicable |
Flash Point(C) | Not applicable |
Purity | ≥98% (HPLC) |
Storage Temp. | −20°C |
UNSPSC | 12352200 |