2. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. Ras Apoptosis
  4. RMC-5127

RMC-5127 is an orally active and brain-penetrant mutant-selective tri-complex RASG12V inhibitor. RMC-5127 non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding . RMC-5127 inhibits the RAS pathway in KRASG12V mutant cancer cells, reducing cell proliferation and inducing apoptosis. RMC-5127 is promising for research of cancers with RAS mutations, such as non-small cell lung cancer.

For research use only. We do not sell to patients.

RMC-5127

RMC-5127 Chemical Structure

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Based on 1 publication(s) in Google Scholar

RMC-5127 Related Antibodies

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K-Ras H-Ras N-Ras Ras

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Description

RMC-5127 is an orally active and brain-penetrant mutant-selective tri-complex RASG12V inhibitor. RMC-5127 non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding . RMC-5127 inhibits the RAS pathway in KRASG12V mutant cancer cells, reducing cell proliferation and inducing apoptosis. RMC-5127 is promising for research of cancers with RAS mutations, such as non-small cell lung cancer[1].

IC50 & Target

KRas G12V

 

Molecular Weight

1062.33

Formula

C57H75N9O9S
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](OC)C1=[C@@]([C@@]2=C(CC(C)(C)COC([C@H]3NN(C([C@@H](NC([C@H]4OC[C@@H]4C)=O)[C@@H]5N6CC7(COC7)C6)=O)C8CC3C8)=O)C9=C(C=CC(C%10=CSC5=N%10)=C9)N2CCOC%11CCOCC%11)C=C(N%12CCN(C%13CC%13)CC%12)C=N1
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 : 125 mg/mL (117.67 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 0.9413 mL 4.7066 mL 9.4133 mL
5 mM 0.1883 mL 0.9413 mL 1.8827 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.19%

SDS (251 KB)

COA (262 KB) HNMR (398 KB) LCMS (343 KB)

Handling Instructions (2659 KB)
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 0.9413 mL 4.7066 mL 9.4133 mL 23.5332 mL
5 mM 0.1883 mL 0.9413 mL 1.8827 mL 4.7066 mL
10 mM 0.0941 mL 0.4707 mL 0.9413 mL 2.3533 mL
15 mM 0.0628 mL 0.3138 mL 0.6276 mL 1.5689 mL
20 mM 0.0471 mL 0.2353 mL 0.4707 mL 1.1767 mL
25 mM 0.0377 mL 0.1883 mL 0.3765 mL 0.9413 mL
30 mM 0.0314 mL 0.1569 mL 0.3138 mL 0.7844 mL
40 mM 0.0235 mL 0.1177 mL 0.2353 mL 0.5883 mL
50 mM 0.0188 mL 0.0941 mL 0.1883 mL 0.4707 mL
60 mM 0.0157 mL 0.0784 mL 0.1569 mL 0.3922 mL
80 mM 0.0118 mL 0.0588 mL 0.1177 mL 0.2942 mL
100 mM 0.0094 mL 0.0471 mL 0.0941 mL 0.2353 mL
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RMC-5127 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:

RMC-5127RMC5127RMC 5127RasApoptosisorally activebrain-penetrantRASG12V(ON)cancersInhibitorinhibitorinhibit

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