2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. MRTX-1257

MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.

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

MRTX-1257 Chemical Structure

MRTX-1257 Chemical Structure

CAS No. : 2206736-04-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 219 In-stock
Solution
10 mM * 1 mL in DMSO USD 219 In-stock
Solid
5 mg USD 176 In-stock
10 mg USD 264 In-stock
25 mg USD 475 In-stock
50 mg USD 688 In-stock
100 mg USD 998 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of MRTX-1257:

MRTX-1257 Related Antibodies

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K-Ras H-Ras N-Ras Ras

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1].

IC50 & Target[1]

KRAS(G12C)

 

Cellular Effect
Cell Line Type Value Description References
NCI-H358 IC50
1 nM
Compound: 19
Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in ERK phosphorylation incubated for 3 hrs by in-cell western method
Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in ERK phosphorylation incubated for 3 hrs by in-cell western method
[PMID: 32250617]
In Vivo

MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) shows rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice[1].
? MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups[1].
? MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained >70 days after cessation of treatment[1].

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

Animal Model: MIA PaCa-2 G12C Xenograft Model (mouse)[1].
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg.
Administration: Orally daily for 30 days.
Result: Showed rapid tumor growth inhibition at all dose groups.
Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups.
100 mg/kg daily led to complete responses that are maintained >70 days after cessation of treatment.
Molecular Weight

565.71

Formula

C33H39N7O2
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

N#CC[C@@H]1N(C(C=C)=O)CCN(C2=C3C(CN(C4=C5C(C)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 55 mg/mL (97.22 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 1.7677 mL 8.8385 mL 17.6769 mL
5 mM 0.3535 mL 1.7677 mL 3.5354 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 (stored under nitrogen). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.42 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.14%

SDS (393 KB)

COA (255 KB) LCMS (267 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 (stored under nitrogen). 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 1.7677 mL 8.8385 mL 17.6769 mL 44.1923 mL
5 mM 0.3535 mL 1.7677 mL 3.5354 mL 8.8385 mL
10 mM 0.1768 mL 0.8838 mL 1.7677 mL 4.4192 mL
15 mM 0.1178 mL 0.5892 mL 1.1785 mL 2.9462 mL
20 mM 0.0884 mL 0.4419 mL 0.8838 mL 2.2096 mL
25 mM 0.0707 mL 0.3535 mL 0.7071 mL 1.7677 mL
30 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.4731 mL
40 mM 0.0442 mL 0.2210 mL 0.4419 mL 1.1048 mL
50 mM 0.0354 mL 0.1768 mL 0.3535 mL 0.8838 mL
60 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7365 mL
80 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5524 mL
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MRTX-1257 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:

MRTX-12572206736-04-9MRTX1257MRTX 1257RasselectivecovalentKRASG12CcancermutantirreversibleERKphosphorylationH358 cellsInhibitorinhibitorinhibit

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