An ALK2 inhibitor
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LDN-212854

Item No. 17698

Technical Information
Formal Name
5-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
CAS Number
1432597-26-6
Molecular Formula
C25H22N6
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 10 mg/mlDMSO: 20 mg/ml
λmax
203, 241, 302 nm
SMILES
N1(C2=CC=C(C(C=N3)=CN4C3=C(C5=C(C=CC=N6)C6=CC=C5)C=N4)C=C2)CCNCC1
InChi Code
InChI=1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2
InChi Key
BBDGBGOVJPEFBT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LDN-212854 inhibits ALK2 (IC50 = 1.3 nM) in preference to other BMP type I receptors, ALK1 (IC50 = 2.4 nM) and ALK3 (IC50 = 85.8 nM) and with over 1,500-fold selectivity against the closely related activin and TGF-β type I receptors (i.e., ALK4 and ALK5).1 It has been shown to inhibit BMP6-induced osteogenic differentiation, which functions predominantly via ALK2, with an IC50 value of 10 nM.1 LDN-212854 also demonstrates off-target activity against RIPK2, ABL1, and PDGFRβ kinases with IC50 values less than 100 nM.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mohedas, A.H., Xing, X., Armstrong, K.A., et alDevelopment of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem. Biol. 8(6), 1291-1302 (2013).