Bioactivity | (R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitory activity against G12D mutated cancer cells[1]. |
Invitro | (R)-G12Di-7 (1-100 nM) 抑制 KRAS-G12D 突变细胞 Ba/F3、SW1990、AsPC-1 和 AGS 的细胞活力,GI50s 分别为 73 nM,409 nM,467 nM 和 109 nM[1]。(R)-G12Di-7 (10 μM) 在 G12D 突变细胞 Ba/F3、SW1990、AsPC-1 和 AGS 中标记 KRAS-G12D,从而抑制下游信号传导,并且在 12 小时之内保持稳定性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> (R)-G12Di-7 相关抗体: Cell Viability Assay[1] Cell Line: |
In Vivo | (R)-G12Di-7 (10-50 mg/kg,腹腔注射,一天两次共 28 天) 在 SW1900 异种移植 NOD/SCID 小鼠体内具有抗肿瘤活性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 2946593-60-6 |
Formula | C39H37F3N6O5 |
Molar Mass | 726.74 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zheng Q, et al., Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D. Nat Chem Biol. 2024 Mar 5. |