2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. (R)-G12Di-7

(R)-G12Di-7 是 KRAS-G12D 的共价配体，可选择性地标记 K-Ras-G12D·GDP 和 K-Ras-G12D·GppNHp。(R)-G12Di-7 对 G12D 突变癌细胞具有抑制活性。

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(R)-G12Di-7 Chemical Structure

(R)-G12Di-7 Chemical Structure

CAS No. : 2946593-60-6

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(R)-G12Di-7 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(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].

体外研究
(In Vitro)

(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，GI50 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.

(R)-G12Di-7 相关抗体:

Cell Viability Assay[1]

Cell Line: Ba/F3, SW1990, AsPC-1, AGS
Concentration: 1-1000 nM
Incubation Time: 72 h
Result: Inhibited cell growth of Ba/F3, SW1990, AsPC-1 and AGS.

Western Blot Analysis[1]

Cell Line: Ba/F3, SW1990, AsPC-1, AGS
Concentration: 10 μM
Incubation Time: 4 h
Result: Suppressed expression K-RAS-G12D and phosphorylation of ERK and Akt in cells G12D mutated cells Ba/F3, SW1990, AsPC-1 and AGS.
体内研究
(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: SW1900 xenograft NOD/SCID mice[1]
Dosage: 10-50 mg/kg
Administration: i.p., twice a day for 28 days
Result: Inhibited tumor growth and weight loss.
分子量

726.74

Formula

C39H37F3N6O5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

(R)-G12Di-7 相关分类

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Keywords:

(R)-G12Di-72946593-60-6RasK-RasG12DBa/F3SW1990AsPC-1AGSNOD/SCIDInhibitorinhibitorinhibit

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