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. Author manuscript; available in PMC: 2013 May 3.

Published in final edited form as: Comb Chem High Throughput Screen. 2011 Sep;14(8):669–687. doi: 10.2174/138620711796504442

Table 4.

Dose-response and solubility of the 12 kinase inhibitors.

Structure	Name	ADP production IC50 (μM)	ADP processing IC50 (μM)	Luminescence detection IC50 (μM)	Solubility	Use/Therapy
	Adaphostin	N.E.¹	N.E.	N.E.	Soluble	BCR-ABL inhibitor; adamantyl ester of tyrphostin AG 957. Shows selective activity against chronic and acute myeloid leukemia. Has not been approved as a drug.
	Dasatinib	N.E.	N.E.	N.E.	Soluble	BCR-ABL inhibitor. A cancer drug Sprycel for use in patients with chronic myelogenous leukemia after imatinib treatment and Philadelphia chromosome-positive acute lymphoblastic leukemia.
	DMPQ	N.E.	N.E.	N.E.	Soluble	PDGFRβ inhibitor. Has not been approved as a drug.
	Erbstatin	N.E.	N.E.	N.E.	Soluble	EGFR inhibitor. Has not been approved as a drug.
	Erk inhibitor	N.E.	N.E.	N.E.	Soluble	Extracellular signal-regulated kinase inhibitor. Has not been approved as a drug.
	Gefitinib	N.E.	N.E.	N.E.	Soluble	EGFR inhibitor. A cancer drug Iressa for use in patients with non-small cell lung cancer with EGFR mutations in Europe, Asia, and Australia.
	Gleevec	N.E.¹	N.E.	N.E.	Soluble	BCR-ABL inhibitor. A cancer drug Imatinib for use in patients with chronic myelogeneous leukemia and gastrointestinal tumors.
	PD 153035	N.E.	N.E.	N.E.	Soluble	EGFR inhibitor, with an IC50 of 25 pM. Inhibits other purified tyrosine kinases only at micromolar or higher concentrations. Has not been approved as a drug.
	PD 169316	N.E.	N.E.	N.E.	Soluble	A selective inhibitor of p38 MAPK; induces apoptosis of neuronal and non-neuronal cells deprived of specific trophic factors. Has not been approved as a drug.
	Phloretin	N.E.	N.E.	N.E.	Soluble	Inhibits glucose transmembrane transport and protein kinase C activity. Induces growth inhibition and apoptosis in human leukemia and colon cancer cells. Has not been approved as a drug.
	SU 4312	N.E.	N.E.	N.E.	Soluble	VEGFR 1/2 and PDGFR inhibitor. Has not been approved as a drug.
	Vatalanib	N.E.	N.E.	N.E.	Soluble	VEGF inhibitor; PTK787. Inhibits angiogenesis. Phase III trials in people with metastatic colorectal cancer. Has not been approved as a drug.

¹

N.E., no effect.