2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. MRTX0902

MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).

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

MRTX0902 Chemical Structure

MRTX0902 Chemical Structure

CAS No. : 2654743-22-1

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Customer Review

Based on 1 publication(s) in Google Scholar

MRTX0902 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10)[1].

IC50 & Target[1]

KRAS-SOS1

46 nM (IC50)

In Vitro

MRTX0902 (compound 32) (1 μM; 0, 2, 4, 8, 15, and 30 minutes) shows a moderate Clint value of 195 mL/min/kg in human liver microsome and a low lipophilicity with cLogP of 3.4[1].
MRTX0902 displays high selectivity on SOS1 (Ki=2 nM) over SOS2 and EGFR (both Ki values >10,000 nM), MRTX0902 inhibits MKN1 cells with an IC50 value of 29 nM[1].

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

MRTX0902 Related Antibodies
In Vivo

MRTX0902 (compound 32) (25, 50 mg/kg; p.o.; twice daily; 25 d) shows anti-tumor effect in mouse model and results tumor regression[1].
MRTX0902 (1-3 mg/kg for i.v. or 10-30 mg/kg for p.o.; single dose) exhibits good brain penetrance, low clearance, and high bioavailability[1].
PK Parameters for MRTX0902 across Species[1]

Parameter Route Dose (mg/kg) Cl (mL/min/kg) Vd,ss (L/kg) T1/2(iv) (h) F (%)
Mouse IV/PO 3/30 4.4 0.28 1.3 69
Rat IV/PO 1/10 14.6 0.28 0.62 83
Dog IV/PO 2/10 7.6 0.48 0.86 38

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

Animal Model: Female CD-1 mice[1]
Dosage: 50 mg/kg
Administration: Oral gavage; twice daily; 1 day
Result: Resulted free drug exposure in the brain as well as the efflux ratio in the Caco-2 assay (ER = 1.5).
Showed short half-life of the compound in mice (T1/2 = 1.3 h).
Animal Model: MIA PaCa-2 xenograft model in mouse[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: Oral gavage; twice daily; 25 days
Result: Reduced tumor growth by 41% and 53% at 25 mg/kg and 50 mg/kg administration.
Clinical Trial
Molecular Weight

388.47

Formula

C22H24N6O
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

C[C@H](C1=C(C(C#N)=CC=C1)C)NC2=NN=C(C)C3=C2C=C(N4CCOCC4)N=C3
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 : 12.5 mg/mL (32.18 mM; ultrasonic and warming and heat to 60°C; 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 2.5742 mL 12.8710 mL 25.7420 mL
5 mM 0.5148 mL 2.5742 mL 5.1484 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)

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (3.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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).
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
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 2.5742 mL 12.8710 mL 25.7420 mL 64.3550 mL
5 mM 0.5148 mL 2.5742 mL 5.1484 mL 12.8710 mL
10 mM 0.2574 mL 1.2871 mL 2.5742 mL 6.4355 mL
15 mM 0.1716 mL 0.8581 mL 1.7161 mL 4.2903 mL
20 mM 0.1287 mL 0.6436 mL 1.2871 mL 3.2178 mL
25 mM 0.1030 mL 0.5148 mL 1.0297 mL 2.5742 mL
30 mM 0.0858 mL 0.4290 mL 0.8581 mL 2.1452 mL
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MRTX0902 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:

MRTX09022654743-22-1MRTX 0902MRTX-0902RasMAPK pathwayKRAS?mutationprotein–protein interactionPPIMRTX849MIA PaCa-2 xenograft modelInhibitorinhibitorinhibit

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