Adagrasib (Synonyms: MRTX849)

Name: Adagrasib
Brand: MedChemExpress
SKU: HY-130149
Rating: 5.0 (41 reviews)

製品番号: HY-130149 純度: 99.81%: Data Sheet SDS COA 取扱説明書
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Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.

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CAS 番号 : 2326521-71-3

容量	価格（税別）	在庫状況	数量
5 mg	USD 74	在庫あり	Estimated Time of Arrival: December 31
10 mg	USD 115	在庫あり	Estimated Time of Arrival: December 31
25 mg	USD 250	在庫あり	Estimated Time of Arrival: December 31
50 mg	USD 450	在庫あり	Estimated Time of Arrival: December 31
100 mg	USD 680	在庫あり	Estimated Time of Arrival: December 31
500 mg	USD 1500	在庫あり	Estimated Time of Arrival: December 31
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Based on 41 publication(s) in Google Scholar

Other Forms of Adagrasib:

MRTX849 analog 24 お問い合わせ
LC-2 お問い合わせ

顧客検証

: Adagrasib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2024 May 8. [Abstract]; Adagrasib (78 nM; 2 h). Cellular activity of KRAS G12C inhibitors in NCI-H358 NSCLC cells was evaluated through active RAS-GTP pull-down followed by immunoblotting using a KRAS-specific antibody after a 2-hour treatment with different inhibitors at indicated concentrations. The levels of active KRAS were quantified by chemiluminescence intensity, and IC50 values were calculated using GraphPad Prism for each compound.

: Adagrasib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Aug 5. [Abstract]; Adagrasib (150 nM, 6-24 h) inhibits KRAS-GTP activity in NCI-H2122 and NCI-H358 cells, but compensatory activation of WT RAS isoforms (including NRAS and MRAS) is observed following monotherapy.

: Adagrasib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Jun;4(6):829-843. [Abstract]; The NCI-H358 KRAS G12C mutant lung cancer cell line was treated with 500 nM adagrasib for 48 hours. Representative immunofluorescence images of E-cadherin are shown. Scale bar, 10 μm.

: Adagrasib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 18.; Adagrasib (MRTX849; 60 nM-1 µM) induces Fas expression in Kras^G12C mutant MIA PaCa-2 cells.

Ras アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

K-Ras H-Ras N-Ras Ras

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

KRas G12C

Cellular Effect

Cell Line	Type	Value	Description	References
AGS	IC₅₀	1.4 μM Compound: MRTX849	Antiproliferative activity against human AGS cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay Antiproliferative activity against human AGS cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay	[PMID: 34965125]
MIA PaCa-2	IC₅₀	4 nM Compound: MRTX849	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay	[PMID: 34965125]
MIA PaCa-2	IC₅₀	5 nM Compound: 20; MRTX849	Inhibition of KRAS G12C mutant in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation incubated for 24 hrs by in-cell western method Inhibition of KRAS G12C mutant in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation incubated for 24 hrs by in-cell western method	[PMID: 32250617]
NCI-H358	IC₅₀	14 nM Compound: 20; MRTX849	Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in ERK phosphorylation incubated for 3 hrs by in-cell western method Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in ERK phosphorylation incubated for 3 hrs by in-cell western method	[PMID: 32250617]
NCI-H358	IC₅₀	6 nM Compound: MRTX849	Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay	[PMID: 34965125]
PaTu 8988t	IC₅₀	3 μM Compound: MRTX849	Antiproliferative activity against human PaTu 8988t cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay Antiproliferative activity against human PaTu 8988t cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay	[PMID: 34965125]

体外実験

Adagrasib (MRTX849) (0.1-10000 nM; 3-day/2D conditions; 12-day/3D conditions) potently inhibits cell growth in the vast majority of KRAS G12C-mutant cell lines with IC₅₀s ranging between 10 and 973 nM in the 2D format and between 0.2 and 1042 nM in the 3D format^[1].
Adagrasib (0.24-1000 nM; 24 hours) inhibits KRAS-dependent signaling targets including ERK1/2 phosphorylation (Thr202/Tyr204 ERK1; pERK), S6 phosphorylation (RSK-dependent Ser235/236; pS6) and expression of the ERK-regulated DUSP6^[1].

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

Cell Viability Assay^[1]

Cell Line:	MIA PaCa-2, H1373, H358, H2122, SW1573, H2030, KYSE-410 cells (G12C); H1299 (WT); A549 (G12S), HCT116 (G13D) cells
Concentration:	0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time:	24 hours
Result:	Inhibits cell growth in the vast majority of KRAS G12C-mutant cell lines with IC₅₀ values ranging between 10 and 973 nM in the 2D format and between 0.2 and 1042 nM in the 3D format.

Western Blot Analysis^[1]

Cell Line:	MIA PaCa-2 cells
Concentration:	0.24, 0.5, 1.0, 2.0, 3.9, 7.8, 15.6, 31.3, 62.5, 125, 250, 500, 1000 nM
Incubation Time:	24 hours
Result:	Inhibits KRAS-dependent signaling targets including ERK1/2 phosphorylation (Thr202/Tyr204 ERK1; pERK), S6 phosphorylation (RSK-dependent Ser235/236; pS6) and expression of the ERK-regulated DUSP6, each with IC₅₀s in the single-digit nanomolar range in cell lines.

体内実験

Adagrasib (1-100 mg/kg; i.g.; daily until day 16) demonstrates dose-dependent anti-tumor efficacy over a well-tolerated dose range, and the maximally efficacious dose of MRTX849 is between 30-100 mg/kg/day^[1].

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

Animal Model:	MIA PaCa-2 model (6-8-week-old, female, athymic nude-Foxn1 nu mice)^[1]
Dosage:	1, 3, 10, 30 and 100 mg/kg
Administration:	Oral gavage; daily until Day 16
Result:	Rapid tumor regression was observed at the earliest posttreatment tumor measurement and animals in the 30 and 100 mg/kg cohorts exhibited evidence of a complete response at study Day 15. Dosing was stopped at study Day 16 and all 4 mice in the 100 mg/kg cohort and 2 out of 7 mice in the 30 mg/kg cohort remained tumor-free through study Day 70.

臨床実験

分子量

604.12

分子式

C₃₂H₃₅ClFN₇O₂

CAS 番号

2326521-71-3

Appearance

Solid

Color

White to yellow

SMILES

N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (41.38 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	1.6553 mL	8.2765 mL	16.5530 mL
5 mM	0.3311 mL	1.6553 mL	3.3106 mL
10 mM	0.1655 mL	0.8277 mL	1.6553 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)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.62 mg/mL (4.34 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.14 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.14 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

mg/kg

Animal weight
(per animal)

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.

純度とドキュメンテーション

純度: 99.81%

Select Batch:

データシート (284 KB) SDS (393 KB)

COA (257 KB) HNMR (278 KB) RP-HPLC (240 KB) LCMS (265 KB) Others (66 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Christensen JG, et al. The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients. Cancer Discov. 2019 Oct 28. pii: CD-19-1167. [Content Brief]

[2]. Kyriakos P. Papadopoulos, et al. A phase I/II multiple expansion cohort trial of MRTX849 in patients with advanced solid tumors with KRAS G12C mutation. Journal of Clinical Oncology 2019 37:15_suppl, TPS3161-TPS3161.

[3]. Fell JB, Fischer JP, Baer BR, et al. Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer. J Med Chem. 2020;63(13):6679-6693. [Content Brief]

[4]. Awad MM, Liu S, Rybkin II, et al. Acquired Resistance to KRASG12C Inhibition in Cancer. N Engl J Med. 2021;384(25):2382-2393. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6553 mL	8.2765 mL	16.5530 mL	41.3825 mL
	5 mM	0.3311 mL	1.6553 mL	3.3106 mL	8.2765 mL
	10 mM	0.1655 mL	0.8277 mL	1.6553 mL	4.1383 mL
	15 mM	0.1104 mL	0.5518 mL	1.1035 mL	2.7588 mL
	20 mM	0.0828 mL	0.4138 mL	0.8277 mL	2.0691 mL
	25 mM	0.0662 mL	0.3311 mL	0.6621 mL	1.6553 mL
	30 mM	0.0552 mL	0.2759 mL	0.5518 mL	1.3794 mL
	40 mM	0.0414 mL	0.2069 mL	0.4138 mL	1.0346 mL

Adagrasib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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.

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Adagrasib (Synonyms: MRTX849)

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Molarity Calculator

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Complete Stock Solution Preparation Table

Adagrasib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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Adagrasib (Synonyms: MRTX849)

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Other Forms of Adagrasib:

Adagrasib 関連抗体

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•関連スクリーニングライブラリ:

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Ras アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Adagrasib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Adagrasib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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