Table 1 Crenolanib and sorafenib in... | American Society of Hematology

Table 1

Crenolanib and sorafenib in vitro kinase binding*

	Crenolanib K_d, nM	Sorafenib K_d, nM
FLT3 variant
FLT3	0.15	13†
FLT3 (ITD)	0.26	95
FLT3 (D835H)	0.16	11
FLT3 (D835Y)	0.14	24
FLT3 (D835V)	3.3	140
FLT3 (ITD, D835V)	3.6	630
FLT3 (ITD, F691L)	22	860
Abl variant		Crenolanib active/inactive Kd ratio
Active Abl	140	0.33
Inactive Abl	430	−
Active Abl (Q252H)	36	0.36
Inactive Abl (Q252H)	100	−

	Crenolanib K_d, nM	Sorafenib K_d, nM
FLT3 variant
FLT3	0.15	13†
FLT3 (ITD)	0.26	95
FLT3 (D835H)	0.16	11
FLT3 (D835Y)	0.14	24
FLT3 (D835V)	3.3	140
FLT3 (ITD, D835V)	3.6	630
FLT3 (ITD, F691L)	22	860
Abl variant		Crenolanib active/inactive Kd ratio
Active Abl	140	0.33
Inactive Abl	430	−
Active Abl (Q252H)	36	0.36
Inactive Abl (Q252H)	100	−

Data obtained from KdELECT screening.

As reported in Davis et al.¹⁷