| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T76024 | ||||
| Target Name | Complement C1s component (C1S) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Cinryze | Drug Info | IC50 = 1.053 U/mL | ||
| Rhucin | Drug Info | IC50 = 1.053 U/mL | |||
| Action against Disease Model | Romiplostim | Drug Info | AMG 531 stimulates murine megakaryopoiesis in vitro by binding to Mpl in the same manner as TPO, via activation of signaling pathways including tyrosine phosphorylation of Mpl, Janus kinase (JAK) 2, and signal transducer and activators of transcription (STAT) 5 14. In vitro studies have also demonstrated that AMG 531 is a potent stimulant of megakaryopoiesis. AMG 531 exerteda dose-dependent effect on the growth of megakaryocytic colony-forming units (CFU-Meg) from murine marrow cells. AMG 531 also stimulated the proliferation of BaF3 cells that expressed h uMan Mpl in adose-dependent fashion, but had no effect on parental BaF3 cells that did not express Mpl. In vitro studies also showed that AMG 531 competes effectively with TPO for binding to h uMan Mpl on normal platelets. | [1] | |
| References | |||||
| REF 1 | AMG 531: an investigational thrombopoiesis-stimulating peptibody. Pediatr Blood Cancer. 2006 Oct 15;47(5 Suppl):723-5. | ||||
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