For research use only. Not for therapeutic Use.
AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity.
AZD7507 (Compound 31) inhibits the proliferation of 3T3 cells engineered to express CSF-1R and stimulated with CSF-1 (IC50, 32 nM), shows inhibitory activity against hERG and NaV1.5, with IC50s of >30 and 26 μM[1].
AZD7507 has good rat oral PK, with in vivo clearance of 7 mL/min/kg and 42% bioavailability. In the canine L-type Ca channel assay, the IC50 is >20 μM[1]. AZD7507 significantly decreases the number of CD68+ macrophages in mice, and also reduces the volume and mass in mice bearing CC-LP-1 and SNU-1079 cells, but not WITT-1 cells[2].
| Catalog Number | I012798 |
| CAS Number | 1041852-85-0 |
| Synonyms | 4-(2-fluoro-4-methylanilino)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-7-methoxycinnoline-3-carboxamide |
| Molecular Formula | C23H27FN6O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H27FN6O3/c1-14-3-4-17(16(24)11-14)26-21-15-12-19(30-7-5-29(6-8-30)9-10-31)20(33-2)13-18(15)27-28-22(21)23(25)32/h3-4,11-13,31H,5-10H2,1-2H3,(H2,25,32)(H,26,27) |
| InChIKey | CPDGCAFPSYOTGO-UHFFFAOYSA-N |
| SMILES | CC1=CC(=C(C=C1)NC2=C(N=NC3=CC(=C(C=C32)N4CCN(CC4)CCO)OC)C(=O)N)F |
| Reference | [1]. Scott DA, et al. Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4591-6. [2]. Boulter L, et al. WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. Send to J Clin Invest. 2015 Mar 2;125(3):1269-85. |
