LC-2 |
| カタログ番号GC61766 |
LC-2 は、0.25 ～ 0.76 μM の DC50 で、内因性 KRAS G12C を分解できる強力なクラス初の von Hippel-Lindau ベースの PROTAC です。 LC-2 は MRTX849 弾頭で KRAS G12C に共有結合し、E3 リガーゼ VHL をリクルートして、ホモ接合型およびヘテロ接合型 KRAS G12C 細胞株の両方で MAPK シグナル伝達の抑制につながる急速かつ持続的な KRAS G12C 分解を誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2502156-03-6
Sample solution is provided at 25 µL, 10mM.
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LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM[1]. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines[2].
LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC50s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via a bona fide PROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h[1].LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines[1]. Western Blot Analysis[1] Cell Line: MIA PaCa-2 cells and NCI-H23 cells
[1]. De Vita E, et al. The Missing Link between (Un)druggable and Degradable KRAS. ACS Cent Sci. 2020;6(8):1281-1284. [2]. Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375.
| Cas No. | 2502156-03-6 | SDF | |
| Canonical SMILES | O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)NC(CCOCCCN4[C@@H](CCC4)COC5=NC(N6C[C@@H](N(CC6)C(C(F)=C)=O)CC#N)=C7C(CN(CC7)C8=C9C(Cl)=CC=CC9=CC=C8)=N5)=O)=O | ||
| Formula | C59H71ClFN11O7S | M.Wt | 1132.78 |
| 溶解度 | DMSO: 50 mg/mL (44.14 mM; ultrasonic and warming and heat to 80°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.8828 mL | 4.4139 mL | 8.8278 mL |
| 5 mM | 0.1766 mL | 0.8828 mL | 1.7656 mL |
| 10 mM | 0.0883 mL | 0.4414 mL | 0.8828 mL |
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Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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