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LY2857785 free base

SIGMA/SML2942 - ≥98% (HPLC)

Synonym: 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

CAS Number: 1619903-54-6
Empirical Formula (Hill Notation): C26H36N6O
Molecular Weight: 448.60
MDL Number: MFCD28167812
Linear Formula: C26H36N6O
Product Type: Chemical

Catalog Number PKG Qty. Price Quantity
45-SML2942-5MG 5 mg
$130.00
1/EA
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45-SML2942-25MG 25 mg
$418.00
1/EA
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assay ≥98% (HPLC)
color white to beige
form powder
Quality Level 100 
SMILES string CN1C(C(C)C)=C2C(C=CC(C3=NC(N[C@H]4CC[C@H](NC5CCOCC5)CC4)=NC=C3)=C2)=N1
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

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