For research use only. Not for therapeutic Use.
Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM)[1].
Golidocitinib (Example 32) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively). Golidocitinib significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells with an IC50 of 161 nM[1].
Golidocitinib (12.5 mg/kg BID (twice daily), 25 m/kg BID or 50 mg/kg BID, p.o.) alone has increasing antitumor effects, and ehances the antitumor activity of osimertinib, compared to treatment with osimertinib alone in mice bearing NCI-H1975 cells[1].
| Catalog Number | I028207 |
| CAS Number | 2091134-68-6 |
| Synonyms | (2R)-N-[3-[2-[(3-methoxy-1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propanamide |
| Molecular Formula | C25H31N9O2 |
| Purity | ≥95% |
| 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 |
| SMILES | CC(C(=O)NC1=CC=CC2=C1NC=C2C3=NC(=NC=C3)NC4=CN(N=C4OC)C)N5CCN(CC5)C |
| Reference | [1]. Annika Birgitta Margareta ÅSTRAND, et al. Compounds and methods for inhibiting jak. WO2017050938A1. |
