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Daraxonrasib
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Catalog No. T74698Cas No. 2765081-21-6
Alias RMC-6236, RMC6236, RAS-IN-2
Daraxonrasib (RMC-6236) is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.
Daraxonrasib
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Purity: 99.98%
Catalog No. T74698Alias RMC-6236, RMC6236, RAS-IN-2Cas No. 2765081-21-6
Daraxonrasib (RMC-6236) is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $55 | In Stock | In Stock | |
| 5 mg | $139 | In Stock | In Stock | |
| 10 mg | $218 | In Stock | In Stock | |
| 25 mg | $375 | In Stock | In Stock | |
| 50 mg | $558 | In Stock | In Stock | |
| 100 mg | $796 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.98%
Appearance:Solid
Color:White to Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Daraxonrasib (RMC-6236)6 is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs. |
| Targets&IC50 | KRAS (WT):154 nM (KD2), KRAS (G12V):131 nM (KD2), CYPA:55.3 nM (KD1), KRas (G12D):364 nM (KD2) |
| In vitro | METHODS: HPAC and Capan-2 cell lines were treated with Daraxonrasib (RMC-6236) (1, 3, 10, 30 nM, 4 hours) and Western Blot analysis was performed.
RESULTS Time- and concentration-dependent inhibition of RAS pathway signaling markers pERK, pAKT, and pS6 were observed in HPAC and Capan-2 cell lines treated with Daraxonrasib (RMC-6236). The inhibition of pERK and pS6 in Capan-2 cells lasted for at least 48 hours. HPAC cells also showed sustained pERK inhibition and time-dependent induction of apoptosis. [1] |
| In vivo | METHODS: Daraxonrasib (RMC-6236) (3, 10, 25 mg/kg, oral) was administered to mice bearing Capan-2 xenograft tumors. The pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of RMC-6236 as well as its antitumor activity in vivo in a range of mutant RAS-driven human tumor xenograft models were evaluated.
RESULTSDaraxonrasib (RMC-6236) exhibited similar PK profiles in multiple xenograft models and did not accumulate in the blood and tumors after repeated dosing; RMC-6236 exposure in various xenograft tumors was approximately 3 to 7 times higher than that in the blood and was cleared relatively slowly from the tumors; consistent with the dose-dependent and prolonged exposure in xenograft tumors, oral administration of RMC-6236 resulted in dose-dependent and persistent inhibition of RAS pathway signaling. [1] |
| Synonyms | RMC-6236, RMC6236, RAS-IN-2 |
| Molecular Weight | 811.05 |
| Formula | C44H58N8O5S |
| Cas No. | 2765081-21-6 |
| Smiles | CCN1C2=C3C=C(C=C2)C4=CSC(=N4)C[C@@H](C(=O)N5CCC[C@H](N5)C(=O)OCC(CC3=C1C6=C(N=CC(=C6)N7CCN(CC7)C)[C@H](C)OC)(C)C)NC(=O)[C@H]8C[C@@H]8C |
| Storage | keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 200 mg/mL (246.59 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 5 mg/mL (6.16 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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