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

(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.

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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 Related Antibodies

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Description

(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].

In Vitro

(R)-G12Di-7 (1-100 nM) inhibits cell viability in KRAS-G12D mutated cells Ba/F3, SW1990, AsPC-1 and AGS with GI50s of 73 nM, 409 nM, 467 nM and 109 nM, respectively[1].
(R)-G12Di-7 (10 μM) labels KRAS-G12D in G12D mutated cells Ba/F3, SW1990, AsPC-1 and AGS, and thus suppresses the downstream signaling with stability over 12 h[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(R)-G12Di-7 Related Antibodies

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.
In Vivo

(R)-G12Di-7 (10-50 mg/kg, twice a day, i.p. for 28 days) exhibits antitumor activity in SW1900 xenograft NOD/SCID mice[1].

MedChemExpress (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.
Molecular Weight

726.74

Formula

C39H37F3N6O5
CAS No.
SMILES

C#CC1=C(C=CC2=CC(O)=CC(C3=C(C4=C(C(N5CC6CCC(N6C([C@@H]7OC(C7(C)C)=O)=O)C5)=NC(OC[C@@]89CCCN8C[C@@H](C9)F)=N4)C=N3)F)=C21)F
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Room temperature in continental US; may vary elsewhere.
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(R)-G12Di-7 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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