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

Olomorasib  (Synonyms: KRAS G12C inhibitor 19)

Cat. No.: HY-132980 Purity: 98.23%
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Olomorasib is a potent inhibitor of KRAS G12C. Olomorasib significantly inhibits tumor growth (extracted from patent WO2021118877A1).

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

Olomorasib Chemical Structure

Olomorasib Chemical Structure

CAS No. : 2771246-13-8

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5 mg USD 240 In-stock
10 mg USD 372 In-stock
25 mg USD 690 In-stock
50 mg USD 1180 In-stock
100 mg USD 2000 In-stock
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Based on 1 publication(s) in Google Scholar

Olomorasib Related Antibodies

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Description

Olomorasib is a potent inhibitor of KRAS G12C. Olomorasib significantly inhibits tumor growth (extracted from patent WO2021118877A1)[1].

IC50 & Target

KRAS G12C[1]
In Vitro

Olomorasib, combined with abemaciclib (HY-16297A), shows IC50 values of 0.001, 0.003 and 0.007 μM for SW1463, H358 and MIAPACA2 cells, respectively[1].

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

Olomorasib Related Antibodies
In Vivo

Olomorasib (12.5-100 mg/kg, single dose) inhibits pERK and KRas in mouse models, showing a time- and dose-dependent effect[1].

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

Animal Model: H358 tumor xenograft mouse model [1]
Dosage: 12.5, 25, 50, 100 mg/kg; 30 mg/kg; single dose
Administration:
Result: Exhibited good inhibition of pERK and active KRas after a single dose treatment from 12.5 to 100 mg/kg. 82.2%-90.6 % pERK inhibition, and 73.4%-94% active KRas inhibition were observed at these dose levels.
Showed at 30 mg/kg, 82.6% pERK inhibition observed at 8 hours, and the pERK inhibition decreased to 65.2% at 24 hours. For active KRas, 80.2% inhibition was achieved at 8 hours, and the active KRas inhibition decreased to 54.9% at 24 hours.
Animal Model: Pancreatic Cancer MiaPaca-2 Xenograft Mouse Model[1]
Dosage: 5, 10, 30 mg/kg; single dose
Administration:
Result: Showed dose and time dependent inhibition of pERK and active KRas in MiaPaca-2 model.
Molecular Weight

528.96

Formula

C25H19ClF2N4O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC=[C@]([C@]2=C(F)C=C(C(N3[C@@](CN(CC3)C(C=C)=O)([H])CCO4)=O)C4=C2Cl)C5=C1SC(N)=C5C#N
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 : 100 mg/mL (189.05 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 1.8905 mL 9.4525 mL 18.9050 mL
5 mM 0.3781 mL 1.8905 mL 3.7810 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 12.5 mg/mL (23.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 12.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (125.0 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: ≥ 12.5 mg/mL (23.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 12.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (125.0 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).
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: 98.41%

SDS (393 KB)

COA (259 KB) HNMR (304 KB) LCMS (112 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 1.8905 mL 9.4525 mL 18.9050 mL 47.2626 mL
5 mM 0.3781 mL 1.8905 mL 3.7810 mL 9.4525 mL
10 mM 0.1891 mL 0.9453 mL 1.8905 mL 4.7263 mL
15 mM 0.1260 mL 0.6302 mL 1.2603 mL 3.1508 mL
20 mM 0.0945 mL 0.4726 mL 0.9453 mL 2.3631 mL
25 mM 0.0756 mL 0.3781 mL 0.7562 mL 1.8905 mL
30 mM 0.0630 mL 0.3151 mL 0.6302 mL 1.5754 mL
40 mM 0.0473 mL 0.2363 mL 0.4726 mL 1.1816 mL
50 mM 0.0378 mL 0.1891 mL 0.3781 mL 0.9453 mL
60 mM 0.0315 mL 0.1575 mL 0.3151 mL 0.7877 mL
80 mM 0.0236 mL 0.1182 mL 0.2363 mL 0.5908 mL
100 mM 0.0189 mL 0.0945 mL 0.1891 mL 0.4726 mL
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Olomorasib 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:

Olomorasib2771246-13-8KRAS G12C inhibitor 19RascancerKRAS G12CKRASInhibitorinhibitorinhibit

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