2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. RM-018

RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRASG12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRASG12C.

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RM-018 Chemical Structure

RM-018 Chemical Structure

CAS No. : 2641993-55-5

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Based on 1 publication(s) in Google Scholar

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Description

RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRASG12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRASG12C[1].

IC50 & Target[1]

KRAS (G12C)

 

KRAS (G12C/Y96D)

 

In Vitro

RM-018 is a “tricomplex” KRAS inhibitor, which exploits a highly abundant chaperone protein, cyclophilin A, to bind and inhibit KRASG12C[1].
? RM-018 (0.01-1000 nM; 72 hours) has IC50s of 1.4-3.5 nM (KRASG12C) and 2.8-7.3 nM (KRASG12C/Y96D) in NCI-H358, MIA PaCa-2, Ba/F3, and MGH1138-1 cells[1].
? RM-018 (0-100 nM; 4 hours) inhibits the expression of KRAS, pERK, and pRSK protein[1].

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

RM-018 Related Antibodies

Cell Viability Assay[1]

Cell Line: NCI-H358, MIA PaCa-2, Ba/F3, and MGH1138-1 cells, which stably infected with KRASG12C or KRASG12C/Y96D.
Concentration: 0.01-1000 nM
Incubation Time: 72 hours
Result: Inhibited the cell activity, but largely unaffected by KRASG12C/Y96D expression.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2, HEK293T and MGH1138-1 cells, which expressing KRASG12C or KRASG12C/Y96D.
Concentration: 0-100 nM
Incubation Time: 4 hours
Result: Inhibited KRAS, pERK and pRSK levels with similar potency.
Molecular Weight

985.22

Formula

C56H72N8O8
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1CCC[C@@H](C(OCC(C)(C)CC2=[C@@]([C@@]3=C([C@H](C)OC)N=CC=C3)N(CC)C4=C2C=C5C=C4)=O)N1)[C@@H](NC([C@H](C(C)C)N(C)C([C@H]6CCN(C(C#CCN7CCOCC7)=O)C6)=O)=O)CC8=CC=CC5=C8
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 60 mg/mL (60.90 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 1.0150 mL 5.0750 mL 10.1500 mL
5 mM 0.2030 mL 1.0150 mL 2.0300 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 1.0150 mL 5.0750 mL 10.1500 mL 25.3750 mL
5 mM 0.2030 mL 1.0150 mL 2.0300 mL 5.0750 mL
10 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5375 mL
15 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
20 mM 0.0508 mL 0.2538 mL 0.5075 mL 1.2688 mL
25 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0150 mL
30 mM 0.0338 mL 0.1692 mL 0.3383 mL 0.8458 mL
40 mM 0.0254 mL 0.1269 mL 0.2538 mL 0.6344 mL
50 mM 0.0203 mL 0.1015 mL 0.2030 mL 0.5075 mL
60 mM 0.0169 mL 0.0846 mL 0.1692 mL 0.4229 mL
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RM-018 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:

RM-0182641993-55-5RM018RM 018RascancerNCI-H358MIA PaCa-2Ba/F3MGH1138-1HEK293T cellsG12CKRASInhibitorinhibitorinhibit

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