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- K-Ras(G12C) inhibitor 12
K-Ras(G12C) inhibitor 12
K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of K-Ras(G12C) [1].
K-Ras is a GTPase and plays an important role in many signal transduction pathways. The mutation of K-Ras occurs in many cancers.
K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of K-Ras(G12C). K-Ras(G12C) exhibited a slight preference for GTP. However, K-Ras(G12C) inhibitor 12 significantly reduced the affinity for GTP and led to the modification of K-Ras(G12C). Also, K-Ras(G12C) inhibitor 12 inhibited SOS-catalysed nucleotide exchange. In H1792 and H358 K-Ras(G12C)-mutant lung cancer cell lines, K-Ras(G12C) inhibitor 12 reduced the association of C-Raf and B-Raf with Ras. In H1792, H358, H23 and Calu-1 cell lines containing G12C mutations, K-Ras(G12C) inhibitor 12 decreased viability and induced apoptosis. K-Ras(G12C) inhibitor 12 exhibited EC50 value of 0.32 μM in H1792 cells. Also, the H1792 cells exhibited low levels of K-Ras GTP, which was consistent with the preference of K-Ras(G12C) inhibitor 12 to K-Ras GDP [1].
Reference:
[1]. Ostrem JM1, Peters U, Sos ML, et al. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature, 2013, 503(7477): 548-551.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 449.67 |
Cas No. | 1469337-95-8 |
Formula | C15H17ClIN3O3 |
Solubility | ≥8.98 mg/mL in DMSO with gentle warming |
Chemical Name | 1-[4-[2-(4-chloro-2-hydroxy-5-iodoanilino)acetyl]piperazin-1-yl]prop-2-en-1-one |
SDF | Download SDF |
Canonical SMILES | C=CC(=O)N1CCN(CC1)C(=O)CNC2=CC(=C(C=C2O)Cl)I |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment[1]: | |
Cell lines |
lung cancer cell lines H23, H358 and H1792 |
Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
72 h, 10 μM |
Applications |
K-Ras(G12C) inhibitor 12 is a highly effective Ras inhibitor and its EC50 value in H1792 cells is 0.32 μM.It selectively binds to an oncogenic mutant K-Ras(G12C) in a irreversible manner without affecting the activity of wild-type Ras. After treatment with K-Ras(G12C) inhibitor 12, K-Ras(G12C)-mutant cells exhibit decreased viability and increased apoptosis comparing to cells lacking this mutation. |
References: [1]. Ostrem J M, Peters U, Sos M L, et al. K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions[J]. Nature, 2013, 503(7477): 548-551. |
Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet