Imara M&A
ELVN-001 is Selective for ABL1
• ELVN-001 has a very selective kinase profile
Clean vs. key off-targets in cells
372 kinases screened at 1 µM compound (100 μM ATP)
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ELVN-001 is also very clean (>10 µM) in an in vitro
safety panel of >130 receptors
ELVN-001
Ponatinib
Nilotinib
Dasatinib
Kinases with >50% inhibition selected for IC50 determination
>100x window vs. all but 2 kinases profiled
Bosutinib
CKIT
>10,000
30
200
0.6
1,000
Cellular Phosphorylation IC50 (nM)
FLT3wt
>10,000
3.8
>10,000
>1,000
4,700
PDGFRb
>10,000
89
720
7.1
7,900
VEGFR2
>10,000
4.8
2,900
>1,000
>10,000
CSRC
>10,000
Reference: Abl kinases are required for vascular function, Tie2, and angiopoietin-1-mediated survival. Pendergast et al. PNAS. 2013;110(30):12432-7.
630
>10,000
10
16
ELVN-001 (100 μM ATP)
Kinase
ABL1
ABL2/ARG
TRKC
TNIK
LOK/STK10
LRRK2
FGR
ACK1
FYN
HGK/MAP4K4
LCK
IC50 (NM)
1
31
41
110
183
486
550
698
725
973
>1,000
Large window for
ABL2/ARG may
result in a
favorable safety
profile
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