For research use only. Not for therapeutic Use.
GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma[1][2].
GNE-9822 (compound 28) inhibits the phosphorylation of PLCγ with an IC50 value of 55 nM[1].
GNE-9822 (compound 28; po and iv; 1 and 5 mg/kg) has good bioavailability and halflives observed in mouse and rats[1].
| Catalog Number | I006991 |
| CAS Number | 1557232-32-2 |
| Synonyms | N-[1-[(1S)-3-(dimethylamino)-1-phenylpropyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamide |
| Molecular Formula | C24H32N6O |
| Purity | ≥95% |
| InChI | InChI=1S/C24H32N6O/c1-24(2)12-10-19-20(14-24)27-28-22(19)23(31)26-18-15-25-30(16-18)21(11-13-29(3)4)17-8-6-5-7-9-17/h5-9,15-16,21H,10-14H2,1-4H3,(H,26,31)(H,27,28)/t21-/m0/s1 |
| InChIKey | XFYUTGIEFKGWND-NRFANRHFSA-N |
| SMILES | CC1(CCC2=C(C1)NN=C2C(=O)NC3=CN(N=C3)C(CCN(C)C)C4=CC=CC=C4)C |
| Reference | [1]. Zhou D, et al. Discovery of Potent and Highly Selective Interleukin-2-Inducible T-Cell Kinase Degraders with In Vivo Activity. J Med Chem. 2023 Apr 13;66(7):4979-4998. [2]. Burch JD, et, al. Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors. J Med Chem. 2014 Jul 10;57(13):5714-27. |
