MRTX-EX185 formic
Based on 1 Customer Validation
MRTX-EX185 formic is a potent KRAS (G12D) inhibitor with an IC50 of 90 nM. MRTX-EX185 formic can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D). MRTX-EX185 formic exhibits broad-spectrum binding properties with IC50s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 formic also binds GDP-loaded HRAS. MRTX-EX185 formic can be used to study various RAS-driven tumors (such as pancreatic cancer) .
For research use only. We do not sell to patients.
- CAS No.: 2988148-70-3
- Formula: C34H35FN6O4
- Molecular Weight:610.68
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
KRas G12D 90 nM (IC50) |
K-Ras WT 110 nM (IC50) |
KRas G12C 290 nM (IC50) |
KRas Q61H 130 nM (IC50) |
KRAS G13D 240 nM (IC50) |
KRas G12V 700 nM (IC50) |
MRTX-EX185 (0.1 nM-100 μM) formic suppresses cell proliferation (IC50 = 70 nM) in KRAS (G12D)-driven SW-1990 pancreatic cancer cells, and is non-toxic to non-KRAS-dependent cell lines (HEK293 cells)[1].
MRTX-EX185 (1 nM-100 μM) formic significantly inhibits ERK phosphorylation (p-ERK) in KRAS(G12C)-driven cell lineages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 2988148-70-3
-
Appearance Solid
-
Molecular Weight 610.68
-
Formula C34H35FN6O4
-
Color Yellow to brown
-
SMILES
OC1=CC(C2=C(F)C3=NC(OCC45CCCN4CCC5)=NC(N6C[C@@](N7)([H])CC[C@@]7([H])C6)=C3C=N2)=C8C(C#C)=CC=CC8=C1.O=CO
-
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
DMSO : 100 mg/mL (163.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.41 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (20.8 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (279 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 1.6375 mL | 8.1876 mL | 16.3752 mL | 40.9380 mL |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2750 mL | 8.1876 mL | |
| 10 mM | 0.1638 mL | 0.8188 mL | 1.6375 mL | 4.0938 mL | |
| 15 mM | 0.1092 mL | 0.5458 mL | 1.0917 mL | 2.7292 mL | |
| 20 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0469 mL | |
| 25 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6375 mL | |
| 30 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3646 mL | |
| 40 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0234 mL | |
| 50 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL | |
| 60 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6823 mL | |
| 80 mM | 0.0205 mL | 0.1023 mL | 0.2047 mL | 0.5117 mL | |
| 100 mM | 0.0164 mL | 0.0819 mL | 0.1638 mL | 0.4094 mL |
MRTX-EX185 formic Related Classifications
HY-145962A Related Classifications
Powered by Bioz