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TL02-59
- Soluble in DMSO
- MF: C32H34F3N5O4
- MW: 609.64
Description
TL02-59 is a potent, selective and orally active inhibitor of Fgr and Lyn kinase with IC50 values of 0.03 nM and 0.10 nM, respectively. TL02–59 exhibits pM potency against the AML-associated Src-family kinase, Fgr, both in vitro and in cell-based kinase assays. TL02–59 inhibited the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. More importantly, TL02–59 induced growth arrest in primary AML bone marrow samples, with Fgr expression correlating most strongly with TL02–59 sensitivity.
More Information
| Parent CAS No. | 1315330-17-6 |
|---|---|
| Chemical Name | 3-(6,7-Dimethoxyquinazolin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide |
| SMILES | C1(C)C=CC(C(=O)NC2C=C(C(F)(F)F)C(CN3CCN(CC)CC3)=CC=2)=CC=1OC1N=CN=C2C=C(OC)C(OC)=CC=12 |
| MFCD | N.A. |
| InChi | InChI=1S/C32H34F3N5O4/c1-5-39-10-12-40(13-11-39)18-22-8-9-23(15-25(22)32(33,34)35)38-30(41)21-7-6-20(2)27(14-21)44-31-24-16-28(42-3)29(43-4)17-26(24)36-19-37-31/h6-9,14-17,19H,5,10-13,18H2,1-4H3,(H,38,41) |
| InChiKey | AMHWQBGAKJESFB-UHFFFAOYSA-N |
| CID | 71254350 |
| Short Description | Fgr/Lyn inhibitor |
References
- L Tan et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.
- MC Weir et al. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 Jun 15;13(6):1551-1559.
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