| Bioactivity | AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity[1]. | ||||||||||||
| Target | IC50: 0.2 nM (Lck), 1 nM (VEGF2), 3 nM (p38α), 72 nM (Jak3), 30 nM (MLR), 21 nM (IL-2) | ||||||||||||
| Name | AMG-47a | ||||||||||||
| CAS | 882663-88-9 | ||||||||||||
| Formula | C29H28F3N5O2 | ||||||||||||
| Molar Mass | 535.56 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem. 2006 Sep 21;49(19):5671-86. [2]. Carver J, et al. A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein. PLoS One. 2014 Aug 5;9(8):e103836. |
AMG-47a
CAS: 882663-88-9 F: C29H28F3N5O2 W: 535.56
AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 n
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