(R)-9b

Names

[ Name ]:
(R)-9b

[Synonym ]:
4-{4-[(5-Chloro-4-{[(2R)-tetrahydro-2-furanylmethyl]amino}-2-pyrimidinyl)amino]phenyl}-1-methylpiperazin-1-ium methanesulfonate
Piperazinium, 4-[4-[[5-chloro-4-[[[(2R)-tetrahydro-2-furanyl]methyl]amino]-2-pyrimidinyl]amino]phenyl]-1-methyl- methanesulfonate (1:1)

Biological Activity

[Description]:

Ack1 inhibitor (R)-9b is a potent and selective ACK1 (TNK2) inhibitor with IC50 of 48 nM; also inhibits JAK2 (IC50=6 nM) and Tyk2 (IC50=5 nM), 3-fold selectvity over ALK and 10-fold over c-Src; potently suppresses proliferation of human cancer cell lines with IC50 <2 uM; exhibits considerable stability in human plasma and a long half-life.

[References]

References 1. Mahajan K, et al. Cancer Cell. 2017 Jun 12;31(6):790-803.e8. 2. Wu X, et al. Oncotarget. 2017 Jan 10;8(2):2971-2983. 3. Lawrence HR, et al. J Med Chem. 2015 Mar 26;58(6):2746-63. View Related Products by Target Ack1 (TNK2)

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₂₇ClN₆O

[ Molecular Weight ]:
499.027

[ Exact Mass ]:
498.181610

Related Compounds

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