tcsc0106 Alisertib

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Product Description

Alisertib (MLN 8237) is a selective Aurora A inhibitor with an IC50 of 1.2 nM.

IC50 & Target: IC50: 1.2 nM (Aurora A)[3]

In Vitro: Alisertib leads the MM cells to mitotic spindle abnormalities, mitotic accumulation, as well as inhibition of cell proliferation through apoptosis and senescence. Alisertib up-regulates p53 and tumor suppressor genes p21 and p27[1]. The decreased activity of MLN8054/Alisertib for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A[2]. Alisertib inhibits cell proliferation with IC50 values ranging from 15 to 469 nM in different tumer cell lines[3].

In Vivo: Alisertib (Alisertib, 30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM[1]. Alisertib (20, 30 mg/kg, p.o.) causes tumor growth inhibition in solid tumor xenograft models and regressions in in vivo models of lymphoma, and reduces FLT uptake in HCT-116 xenograft tumors[3].

Information

CAS No1028486-01-2
FormulaC27H20ClFN4O4
Clinical Informationclinicalinformation
PathwayCell Cycle/DNA Damage
Epigenetics
Autophagy
TargetAurora Kinase
Aurora Kinase
Autophagy

Specifications

Purity / Grade>98%
SolubilityDMSO : 9.33 mg/mL (17.98 mM; Need ultrasonic and warming)
Smilessmiles

Misc Information

Alternative NamesMLN 8237
Observed Molecular Weight518.92
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