LY2874455
LY2874455
CAS: 1254473-64-7
Molecular Formula: C21H19Cl2N5O2
LY2874455 - Names and Identifiers
LY2874455 - Physico-chemical Properties
| Molecular Formula | C21H19Cl2N5O2 |
| Molar Mass | 444.31 |
| Density | 1.44 |
| Boling Point | 672.6±55.0 °C(Predicted) |
| Solubility | DMSO |
| pKa | 12.93±0.40(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | LY2874455 inhibited FGF/FGFR-mediated signaling activity in RT-112 cells, HUVECs,KATO-III cells, and SNU-16 cells. LY2874455 showed FGFR-dependent anti-proliferative effects in KMS-11,OPM-2,SNU-16 and KATO-III cells. LY2874455 inhibits FGF/FGFR-mediated signaling activity in RT-112 cells, HUVECs,KATO-III cells, and SNU-16 cells. LY2874455 showed FGFR-dependent anti-proliferative effects in KMS-11,OPM-2,SNU-16 and KATO-III cells. |
| In vivo study | In mouse heart tissue, LY2874455 exhibited potent inhibition of FGF-induced Erk phosphorylation with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively. LY2874455 (3 mg/kg p.o.) dose-dependently inhibited tumor growth in mice bearing RT-112,OPM-2 (DSMZ),SNU-16, or NCI-H460 xenografts. in mouse heart tissue, LY2874455 exhibited potent inhibition of FGF-induced Erk phosphorylation with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively. LY2874455 (3 mg/kg p.o.) dose-dependently inhibited tumor growth in mice bearing RT-112,OPM-2 (DSMZ),SNU-16, or NCI-H460 xenografts. |
LY2874455 - Introduction
LY2874455 is a pan-FGFR inhibitor with IC50 values for FGFR1,FGFR2, FGFR3, and FGFR4 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM, respectively. And can also inhibit the activity of VEGFR2, IC50 is 7 nM. Phase 1.
Last Update：2022-10-16 17:41:22
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View History
LY2874455
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