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Merck

SML2678

Sigma-Aldrich

A-770041

≥98% (HPLC)

Sinónimos:

A 770041, A770041, N-[4-[1-[trans-4-(4-Acetyl-1-piperazinyl)cyclohexyl]-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-1-methyl-1H-indole-2-carboxamide, trans-KIN 001-111

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About This Item

Fórmula empírica (notación de Hill):
C34H39N9O3
Número de CAS:
Peso molecular:
621.73
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Análisis

≥98% (HPLC)

formulario

powder

color

white to beige

solubilidad

DMSO: 2 mg/mL, clear

temp. de almacenamiento

−20°C

cadena SMILES

NC1=NC=NC2=C1C(C3=CC=C(NC(C4=CC(C=CC=C5)=C5N4C)=O)C(OC)=C3)=NN2[C@@H]6CC[C@@H](N7CCN(C(C)=O)CC7)CC6

InChI

1S/C34H39N9O3/c1-21(44)41-14-16-42(17-15-41)24-9-11-25(12-10-24)43-33-30(32(35)36-20-37-33)31(39-43)23-8-13-26(29(19-23)46-3)38-34(45)28-18-22-6-4-5-7-27(22)40(28)2/h4-8,13,18-20,24-25H,9-12,14-17H2,1-3H3,(H,38,45)(H2,35,36,37)

Clave InChI

ZMNWFTYYYCSSTF-UHFFFAOYSA-N

Acciones bioquímicas o fisiológicas

A-770041 is an orally available (rat F = 34.1%; 10 mg/kg p.o.), ATP-competitive, potent and selctive Lck inhibtor (IC50 = 147 nM/Lck, 1.18 μM/Lyn, 1.22 μM/Hck, 9.05 μM/Src, 14.1 μM/Fgr, 44.1 μM/Fyn; >25 μM/IKK1, IKK2, IRAK4, p38, JAK3, ZAP70, ITK, PKC, MK2, PKA, TYK2, COT,Syk; >50 μM/Tie-2 & Kdr; 1 mM ATP). A-770041 inhibits CD3 mAb-induced IL-2 production in human whole blood in vitro (IC 50 = 80 nM) and in mice in vivo (IC50 = 78 nM plasma conc.), and significantly lengthens graft survival time in a rat heterotopic heart transplant model (2.5 & 5 mg/kg bid p.o.).

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)

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Researchers have shown that the level of immunoglobulin D (IgD) is often elevated in patients with autoimmune diseases. The possible roles of IgD on the function of human T cell activation are still unclear. Paeoniflorin-6'-O-benzene sulfonate (code: CP-25), the chemistry
Andrew Burchat et al.
Bioorganic & medicinal chemistry letters, 16(1), 118-122 (2005-10-12)
We describe the identification, SAR, and pharmacology of the src-family selective lck inhibitor A-770041 that prolongs the survival of major histocompatibility mismatched allografts in models of solid organ transplant rejection for greater than 65 days.
X Li et al.
Allergy, 73(2), 361-368 (2017-09-01)
In mast cells, induction of HSP70 expression during antigen stimulation has not been reported. Mouse bone marrow-derived mast cells (BMMC) were stimulated with IgE/Ag or HSP70. Induction of HSP70 expression and signaling protein phosphorylation were evaluated by immunoblotting. HSP70 expression
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Reversing multidrug resistance (MDR) has been an important goal for clinical and investigational oncologists. In the last few decades, significant effort has been made to search for inhibitors to reverse MDR by targeting ATP-binding cassette (ABC) transporters (Pgp, MRP) directly

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