LC 2 is a mutant-selective PROTAC™ Degrader of KRAS, comprising a ligand for the von Hippel Lindau E3 ligase joined to the KRAS inhibitor MRTX849. LC 2 induces selective degradation of KRASG12C in cancer cell lines without inducing degradation of any other mutants (DC50 = 0.25-0.76 μM), leading to suppression of MAPK signaling and modulation of ERK signaling in both homozygous and heterozygous KRASG12C cancer cell lines. LC 2 inhibits phosphorylation of ERK in SW1573 cell lines.
Negative control LC 2 Epimer (Cat. No. 7421) also available.
PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-125780 |
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| Réf. fabricant | 18776556 |
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| Nom chimique ou matériau | (2 S,4 R)-1-(-2-(3-(3-(-2-(((7-(8-Chloronaphthalen-1-yl)-4-(-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-m) |
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| CAS | 2502156-03-6 |
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| Quantité | 2 mg |
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| Cible | Active Degraders |
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| Formule moléculaire | C<sub>59</sub>H<sub>71</sub>ClFN<sub>11</sub>O<sub>7</sub>S |
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| Pureté | 0.95 |
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