Tozasertib

Research use only, not for human use.

Tozasertib (MK-0457, VX-680) is a highly potent, selective and reversible Aurora kinase inhibitor with Ki of 0.6, 18 and 4.6 nM for Aurora A, B and C, respectively.

Tozasertib (MK-0457, VX-680) is a highly potent, selective and reversible Aurora kinase inhibitor with Ki of 0.6, 18 and 4.6 nM for Aurora A, B and C, respectively; also inhibits the imatinib-resistant ABL(T315I) kinase with Kd of 5 nM, displays >100-fold selectivity for the Aurora-A kinase over 55 other kinases with the only exception FLT-3 (Ki=30 nM); blocks cell-cycle progression and induces apoptosis in a diverse range of human tumor types; causes profound inhibition of tumor growth in a variety of in vivo xenograft models.Blood Cancer Discontinued.

——

——

MK-0457 | VX-680 | MK0457 | VX680 | VX 680 | MK 0457

Cell Cycle/DNA Damage

Aurora Kinase

AuroraA|AuroraB|AuroraC|Bcr-Abl|FLT3

Cancer

Blood cancer

639089-54-6

464.5864

C23H28N8OS

>98% (HPLC)

10 mM in DMSO

O=C(C1CC1)NC2=CC=C(SC3=NC(NC4=CC(C)=NN4)=CC(N5CCN(C)CC5)=N3)C=C2

Cyclopropanecarboxamide, N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years