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LDN 212854 trihydrochloride
- Parent CAS: 1432597-26-6
- Soluble in water and DMSO
- MF: C25H22N6.3HCl
- MW: 515.87
Description
Potent ALK2-biased BMP type I receptor kinase inhibitor (IC50 values 2.4 nM, 1.3 nM, and 85.8 nM for ALK1, 2, and 3 resp.), showing nearly 4 orders of selectivity for BMP versus the closely related TGF-β and Activin type I receptors. The free base form, LDN 212854 is available as Axon 3552. Closely related to LDN 193189 (Axon 1509).
More Information
| Parent CAS No. | 1432597-26-6 |
|---|---|
| Chemical Name | 5-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline trihydrochloride |
| SMILES | N1C2C(=C(C3=C4N(N=C3)C=C(C3=CC=C(N5CCNCC5)C=C3)C=N4)C=CC=2)C=CC=1.Cl.Cl.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C25H22N6.3ClH/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;3*1H |
| InChiKey | RIMSXBSYXNLYPT-UHFFFAOYSA-N |
| CID | 91826503 |
| Short Description | BMP inhibitor |
References
- A.H. Mohedas et al. Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. ACS Chem. Biol. 2013. [Epub ahead of print].
- D.W. Engers et al. Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of (...). Bioorg. Med. Chem. Lett. 2013, 23, 3248-3252.
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