| Identification | Back Directory | [Name]
(R)-9b
(Ack1 inhibitor (R)-9b) | [CAS]
1655527-68-6 | [Synonyms]
Ack1 inhibitor (R)-9b
(R)-9b
(Ack1 inhibitor (R)-9b)
2,4-Pyrimidinediamine, 5-chloro-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N4-[[(2R)-tetrahydro-2-furanyl]methyl]- | [Molecular Formula]
C20H27ClN6O | [MOL File]
1655527-68-6.mol | [Molecular Weight]
402.92 |
| Chemical Properties | Back Directory | [Boiling point ]
617.8±65.0 °C(Predicted) | [density ]
1.289±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
7.87±0.42(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
(R)-9b is a potent inhibitor of ACK1 tyrosine kinase (IC50=56 nM) with anticancer activity. (R)-9b exhibits selectivity for ACK1 but has inhibitory effects on JAK family kinases JAK2 and Tyk2. (R)-9b can be used in the study of hormone-regulated cancers such as prostate and breast cancer[1]. | [Biological Activity]
(R)-9bMS is a potent and selective inhibitor of ACK1 (TNK2) tyrosine kinase th at exhibits potent anticancer activity. (R)-9bMS attenuates AR and AR-V7 expression in prostate cancer cells. (R)-9bMS potently inhibits triple negative breast cancer (TNBC) cells proliferation. | [IC 50]
JAK2; Tyk2 | [References]
[1] Lawrence H R, et al. Development of novel ACK1/TNK2 inhibitors using a fragment-based approach[J]. Journal of medicinal chemistry, 2015, 58(6): 2746-2763. DOI:10.1021/jm501929n |
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