Description
AT9283 can inhibit Aurora A Kinase, Aurora B Kinase, JAK3, JAK2, and Abl with IC50 of 3 nM, 3 nM, 1.1 nM, 1.2 nM and 4 nM.
Storage
2 years at -20centigrade Powder
Targets
Aurora A, Aurora B, JAK3, JAK2, Abl
Molecular Formula
C19H23N7O2
Chemical Name
1-cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)urea
Solubility
DMSO 76 mg/mL Water
In vitro
AT9283 can potently inhibit aurora kinase A and aurora kinase B with around 3 nM, both of which play a key role in regulating mitotic division and are attractive oncology targets. For cell lines (1)AT9283 potently inhibited proliferation and Jak2-related signalling in Jak2-dependent cell lines as well as inhibiting the formation of erythroid colonies from haematopoietic progenitors isolated from MPD patients with Jak2 mutations. (2)Besides inhibition to JAK, AT9283 also act as an aurora inhibitor. And exposure to AT9283 for one complete cell cycle committed an entire population of p53 checkpoint-compromised cells (HCT116) to multinucleation and death whereas treatment of p53 checkpoint-competent cells (HMEC, A549) for a similar length of time led to a reversible arrest of cells with 4N DNA. (3) AT9283 showed potent antiproliferative activity on cells transformed by wild-type BCR-ABL and BCR-ABL/T315I. AT9283 inhibited proliferation in a panel of BaF3 and human BCR-ABL(+) cell lines both sensitive and resistant to imatinib because of a variety of mechanisms.
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