AZD-4205
- Golidocitinib
- Optical Purity: 100% e.e.
- Soluble in DMSO
- MF: C25H31N9O2
- MW: 489.57
Description
AZD-4205 is a potent, selective and ATP-competitive inhibitor of JAK1 with a Ki of 2.8 nM, highly selective against JAK2 (IC50 =13233 nM, >4000 fold selectivity) and JAK3 (IC50 >30000 nM, >10000 fold selectivity). Demonstrates potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome. Exhibits excellent pharmacokinetics, and in vitro and in vivo antitumor efficacy.
More Information
| Parent CAS No. | 2091134-68-6 |
|---|---|
| Chemical Name | (R)-N-(3-(2-(3-Methoxy-1-methyl-1H-pyrazol-4-ylamino)pyrimidin-4-yl)-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12C(NC([C@@H](C)N3CCN(C)CC3)=O)=CC=CC=1C(C1C=CN=C(NC3C(OC)=NN(C)C=3)N=1)=CN2 |&1:4,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C25H31N9O2/c1-16(34-12-10-32(2)11-13-34)23(35)28-20-7-5-6-17-18(14-27-22(17)20)19-8-9-26-25(29-19)30-21-15-33(3)31-24(21)36-4/h5-9,14-16,27H,10-13H2,1-4H3,(H,28,35)(H,26,29,30)/t16-/m1/s1 |
| InChiKey | CVCVOSPZEVINRM-MRXNPFEDSA-N |
| CID | 126715380 |
| Short Description | JAK1 inhibitor |
References
- Q Su et al. Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor. J Med Chem. 2020 May 14;63(9):4517-4527.
- V Chaturvedi et al.JAK inhibition for murine HLH requires complete blockade of IFN-γ signaling and is limited by toxicity of JAK2 inhibition. Blood. 2021 Sep 23;138(12):1034-1039.
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