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SML2942

Sigma-Aldrich

LY2857785 free base

≥98% (HPLC)

Sinónimos:

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

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About This Item

Fórmula empírica (notación de Hill):
C26H36N6O
Número de CAS:
1619903-54-6
Peso molecular:
448.60
Número MDL:
MFCD28167812
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

100

Análisis

≥98% (HPLC)

formulario

powder

color

white to beige

solubilidad

DMSO: 2 mg/mL, clear

temp. de almacenamiento

−20°C

cadena SMILES

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-

Clave InChI

LHIUZPIDLZYPRL-MXVIHJGJSA-N

Acciones bioquímicas o fisiológicas

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.

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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James Bogenberger et al.
Oncotarget, 8(63), 107206-107222 (2018-01-02)
More effective treatment options for elderly acute myeloid leukemia (AML) patients are needed as only 25-50% of patients respond to standard-of-care therapies, response duration is typically short, and disease progression is inevitable even with some novel therapies and ongoing clinical
Jiali Ou et al.
Biochemical and biophysical research communications, 513(4), 967-973 (2019-04-22)
Circadian clock and cell cycle are vital cellular programs acting in a timely-regulated, cyclic manner. The two cellular oscillators are coupled in various ways to facilitate biological processes. Here we report CDK9, a kinase belongs to the CDK family in
Tinggui Yin et al.
Molecular cancer therapeutics, 13(6), 1442-1456 (2014-04-02)
DNA-dependent RNA polymerase II (RNAP II) largest subunit RPB1 C-terminal domain (CTD) kinases, including CDK9, are serine/threonine kinases known to regulate transcriptional initiation and elongation by phosphorylating Ser 2, 5, and 7 residues on CTD. Given the reported dysregulation of
Qi Xie et al.
The Journal of clinical investigation, 126(7), 2757-2772 (2016-06-21)
Glioblastomas co-opt stem cell regulatory pathways to maintain brain tumor-initiating cells (BTICs), also known as cancer stem cells. NOTCH signaling has been a molecular target in BTICs, but NOTCH antagonists have demonstrated limited efficacy in clinical trials. Recombining binding protein
Natalia J Martinez et al.
Scientific reports, 8(1), 9472-9472 (2018-06-23)
Assessment of the interactions between a drug and its protein target in a physiologically relevant cellular environment constitutes a major challenge in the pre-clinical drug discovery space. The Cellular Thermal Shift Assay (CETSA) enables such an assessment by quantifying the
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