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

(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.
Appearance

Solid

Color

White to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (68.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3760 mL 6.8800 mL 13.7601 mL
5 mM 0.2752 mL 1.3760 mL 2.7520 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3760 mL 6.8800 mL 13.7601 mL 34.4002 mL
5 mM 0.2752 mL 1.3760 mL 2.7520 mL 6.8800 mL
10 mM 0.1376 mL 0.6880 mL 1.3760 mL 3.4400 mL
15 mM 0.0917 mL 0.4587 mL 0.9173 mL 2.2933 mL
20 mM 0.0688 mL 0.3440 mL 0.6880 mL 1.7200 mL
25 mM 0.0550 mL 0.2752 mL 0.5504 mL 1.3760 mL
30 mM 0.0459 mL 0.2293 mL 0.4587 mL 1.1467 mL
40 mM 0.0344 mL 0.1720 mL 0.3440 mL 0.8600 mL
50 mM 0.0275 mL 0.1376 mL 0.2752 mL 0.6880 mL
60 mM 0.0229 mL 0.1147 mL 0.2293 mL 0.5733 mL
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(R)-G12Di-7 Related Classifications

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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