製品番号: HY-148439

Daraxonrasib

(別名: RMC-6236; RAS-IN-2)

17 Cited Publications

カスタマーレビュー

Based on 17 publication(s) in Google Scholar

Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC₅₀ values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.96%
CAS 番号: 2765081-21-6
分子式: C₄₄H₅₈N₈O₅S
分子量:811.05

保管条件:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Daraxonrasib 構造式

CAS 番号: 2765081-21-6

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (17)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

KRas G12D

Ras アイソフォーム固有の製品をすべて表示 :

体外実験

Daraxonrasib (EC₅₀ of 1.2 nM for HPAC cells and 1.4 nM for Capan-2 cells; 120 h) potently inhibits the growth of KRAS mutant cancer cell lines HPAC and Capan-2^[1].
Daraxonrasib (10 nM; 0-48 h) cannot durably inhibit mTOR activity when used alone in GP2D colorectal cancer cells, but it can control the rebound of mTOR activity when combined with KO-2806^[2].

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

体内実験

Daraxonrasib (3-25 mg/kg; p.o.; single dose) shows dose-dependent blood and tumor exposure in the Capan-2 xenograft tumor-bearing BALB/c nude mouse model, with tumor exposure approximately 3-7 times higher than that in blood and relatively slower elimination from tumors^[1].
Daraxonrasib (10-25 mg/kg; p.o.; once daily; 4 weeks) shows dose-dependent antitumor activity in a series of human tumor xenograft models harboring prevalent KRAS mutations (such as Capan-2, NCI-H441, HPAC, NCI-H358, etc.)^[1].
Daraxonrasib (25 mg/kg; p.o.; once daily) can arrest tumor growth when used alone in xenograft models of KRAS^G12C-mutant NCI-H2122 non-small cell lung cancer and KRAS^G12D-mutant GP2D colorectal cancer, and it can lead to significant tumor regression when combined with KO-2806^[2].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 2765081-21-6
性状 Solid
分子量 811.05
分子式 C₄₄H₅₈N₈O₅S
Color White to off-white
SMILES

O=C([C@H]1NN(C([C@H](CC2=NC3=CS2)NC([C@H]4C[C@@H]4C)=O)=O)CCC1)OCC(C)(C)CC5=[C@@](N(CC)C6=C5C=C3C=C6)[C@@]7=C([C@H](C)OC)N=CC(N8CCN(C)CC8)=C7
別名

RMC-6236; RAS-IN-2
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (17)

All Cell Proliferation/Viability AssayCell Migration/Invasion AssayWBGel Electrophoresis

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Journal Impact Factor

Nature

Cytosolic acetyl-coenzyme A is a signalling metabolite to control mitophagy. [Abstract]

2026 Jan;649(8098):1022-1031. PMID: 41225001
Cancer Res

Prolonged KRAS-MAPK Inhibition Induces Interferon Signaling That Promotes Cell State Transition and Confers Therapeutic Vulnerabilities. [Abstract]

2026 Jul 2;86(13):3270-3286. PMID: 42008116
Cancer Res

Combination of the MTA-Cooperative PRMT5 Inhibitor BMS-986504 and KRAS Inhibitors is an Effective Treatment Strategy for MTAP-Deleted KRAS-Mutant Pancreatic Cancer. [Abstract]

2025 Jul 22. PMID: 40694535
Cancer Res

A Pan-RAS Inhibitor with a Unique Mechanism of Action Blocks Tumor Growth and Induces Antitumor Immunity in Gastrointestinal Cancer. [Abstract]

2025 Mar 3;85(5):956-972. PMID: 39700396
J Adv Res

Targeting class I HDACs suppresses oncogenic vulnerabilities and potentiates KRAS/MAPK pathway inhibitors in KRAS-mutant cancers. [Abstract]

2026 Feb 13:S2090-1232(26)00144-X. PMID: 41692243
EBioMedicine

A bedside-to-bench translational analysis of NF1 alterations and CDK4/6 inhibitor resistance in hormone receptor-positive metastatic breast cancer. [Abstract]

2025 Aug:118:105828. PMID: 40578027
PLoS One

Daraxonrasib, a pan-RAS inhibitor, selectively inhibits osteosarcomas with activated KRAS by halting AKT signaling and matrix metalloprotease activity. [Abstract]

2025 Aug 8;20(8):e0329946. PMID: 40779492

Daraxonrasib purchased from MedChemExpress. Usage Cited in: PLoS One. 2025 Aug 8;20(8):e0329946. [Abstract]

Proliferation assay of treatment with DMSO or Daraxonrasib (5 nM; 3 days) in HOS and 143B cell lines.

Daraxonrasib purchased from MedChemExpress. Usage Cited in: PLoS One. 2025 Aug 8;20(8):e0329946. [Abstract]

HOS-143B cells were seeded in 96-well plates, scratched with a 200 µl pipette tip, and then incubated overnight with DMSO or Daraxonrasib (5 nM and 10 nM). Medium containing 0.1% serum was used as a negative control.

Daraxonrasib purchased from MedChemExpress. Usage Cited in: PLoS One. 2025 Aug 8;20(8):e0329946. [Abstract]

HOS-143B cells were treated with daraxonrasib (5 nM and 10 nM; 24 h) . Daraxonrasib treatment downregulated ERK1/2 phosphorylation.

Daraxonrasib purchased from MedChemExpress. Usage Cited in: PLoS One. 2025 Aug 8;20(8):e0329946. [Abstract]

Gelatin zymography demonstrated that Daraxonrasib (5 nM and 10 nM; 48 h) inhibited MMP1 activity in HOS-143B cells.
Georgetown University

2026.
bioRxiv

Mono-ADP-ribosylation-driven immunosuppression and cross-resistance to therapy through cancer cell intrinsic and extrinsic mechanisms. [Abstract]

2026 Jun 3:2026.06.01.729331. PMID: 42282595
bioRxiv

2026 Jun 25.
bioRxiv

2026 Apr 6.
bioRxiv

Characterization and therapeutic suppression of KEAP1-NRF2-driven resistance to KRAS inhibitors in pancreatic and lung cancer. [Abstract]

2026 Apr 21:2026.04.18.719329. PMID: 42079131
medRxiv

2026 Apr 18.
bioRxiv

2026 Mar 12.
bioRxiv

2026 Feb 2.
bioRxiv

Prevalence and Actionability of MTAP Loss in Oncogene-Driven Lung Cancer. [Abstract]

2026 Jan 23:2026.01.21.700721. PMID: 41648424
bioRxiv

Phosphorylation Protects Oncogenic RAS from LZTR1-Mediated Degradation. [Abstract]

2026 Jan 7:2026.01.07.698128. PMID: 41542462

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (123.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2330 mL

6.1648 mL

12.3297 mL

5 mM

0.2466 mL

1.2330 mL

2.4659 mL

10 mM

0.1233 mL

0.6165 mL

1.2330 mL

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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

Stock Solution Working Solution

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 (3.08 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.

Protocol 2

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

Solubility: 2.5 mg/mL (3.08 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Jiang J, et al. Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers. Cancer Discov. 2024 Jun 3;14(6):994-1017. [Content Brief]

[2]. Patel H V, et al. The farnesyl transferase inhibitor KO-2806 re-sensitizes relapsing tumors to RAS inhibition. BioRxiv, 2024: 2024.12. 20.629824.

[3]. Long SA, et al. Evaluation of KRAS inhibitor-directed therapies for pancreatic cancer treatment. Front Oncol. 2024 May 10;14:1402128. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.2330 mL	6.1648 mL	12.3297 mL	30.8242 mL
	5 mM	0.2466 mL	1.2330 mL	2.4659 mL	6.1648 mL
	10 mM	0.1233 mL	0.6165 mL	1.2330 mL	3.0824 mL
	15 mM	0.0822 mL	0.4110 mL	0.8220 mL	2.0549 mL
	20 mM	0.0616 mL	0.3082 mL	0.6165 mL	1.5412 mL
	25 mM	0.0493 mL	0.2466 mL	0.4932 mL	1.2330 mL
	30 mM	0.0411 mL	0.2055 mL	0.4110 mL	1.0275 mL
	40 mM	0.0308 mL	0.1541 mL	0.3082 mL	0.7706 mL
	50 mM	0.0247 mL	0.1233 mL	0.2466 mL	0.6165 mL
	60 mM	0.0205 mL	0.1027 mL	0.2055 mL	0.5137 mL
	80 mM	0.0154 mL	0.0771 mL	0.1541 mL	0.3853 mL
	100 mM	0.0123 mL	0.0616 mL	0.1233 mL	0.3082 mL

Keywords

Daraxonrasib

17 Cited Publications

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Daraxonrasib

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High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

KRAS Targeted Compound Library

MedChemExpress（MCE）の使用を引用している文献 Daraxonrasib

Ras アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (17)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Daraxonrasib 関連分類

HY-148439 関連分類