Cat. No.: HY-130149

Adagrasib

(Synonyms: MRTX849)

63 Cited Publications

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Based on 63 publication(s) in Google Scholar

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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Pureté: 99.96%
CAS No.: 2326521-71-3
Formule: C₃₂H₃₅ClFN₇O₂
Masse moléculaire:604.12

Stockage:

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

Adagrasib Chemical Structure

CAS No.: 2326521-71-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (63)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

KRas G12C

Voir tous les produits spécifiques à Isoform Ras :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	12.9 μM Compound: 3; MRTX849	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell proliferation incubated for 3 days by CCK8 assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell proliferation incubated for 3 days by CCK8 assay	[PMID: 36395648]
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	0.05 μM Compound: 3; MRTX849	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell proliferation incubated for 3 days by CCK8 assay Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell proliferation incubated for 3 days by CCK8 assay	[PMID: 36395648]
MIA PaCa-2	IC₅₀	0.1 μM Compound: 17, MRTX849	Antiproliferative activity against human MIA PaCa-2 cells Antiproliferative activity against human MIA PaCa-2 cells	[PMID: 32910655]
MIA PaCa-2	IC₅₀	3.92 nM Compound: MRTX849	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by cell count reagent SF based assay Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by cell count reagent SF based assay	[PMID: 37393576]
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-H1975	IC₅₀	6.37 μM Compound: 3; MRTX849	Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as inhibition of cell proliferation incubated for 3 days by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as inhibition of cell proliferation incubated for 3 days by CCK8 assay	[PMID: 36395648]
NCI-H358	IC₅₀	0.001 μM Compound: MRTX-849	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell growth Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell growth	[PMID: 36621179]
NCI-H358	IC₅₀	0.006 μM Compound: 2	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay	[PMID: 37395055]
NCI-H358	IC₅₀	0.02 μM Compound: 3; MRTX849	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell proliferation incubated for 3 days by CCK8 assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell proliferation incubated for 3 days by CCK8 assay	[PMID: 36395648]
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]
NCI-H358	IC₅₀	9.2 nM Compound: MRTX849	Antiproliferative activity against human NCI-H358 cells harboring KRAS p.G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by cell count reagent SF based assay Antiproliferative activity against human NCI-H358 cells harboring KRAS p.G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by cell count reagent SF based assay	[PMID: 37393576]
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]

In Vitro

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.

In Vivo

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.

Essai clinique

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

Chemical Information

CAS No. 2326521-71-3
Appearance Solid
Masse moléculaire 604.12
Formule C₃₂H₃₅ClFN₇O₂
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
Synonyms

MRTX849
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (63)

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Journal Impact Factor

Ann Oncol

Genomic landscape of clinically acquired resistance alterations in patients treated with KRASG12C inhibitors. [Abstract]

2025 Jun;36(6):682-692. PMID: 39914665
Nature

Antibodies against endogenous retroviruses promote lung cancer immunotherapy. [Abstract]

2023 Apr;616(7957):563-573. PMID: 37046094
Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
Cancer Cell

A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]

2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213
Cancer Cell

KRASG12D inhibition reprograms the microenvironment of early and advanced pancreatic cancer to promote FAS-mediated killing by CD8+ T cells. [Abstract]

2023 Sep 11;41(9):1606-1620.e8. PMID: 37625401
Cancer Discov

EML4-ALK mediates resistance to KRAS G12C inhibition and induces an oncogenic dependency by rewiring signaling through the wild-type RAS pathway. [Abstract]

2026 Jun 22. PMID: 42329099
Cancer Discov

Epigenetic and oncogenic inhibitors cooperatively drive differentiation and kill KRAS-mutant colorectal cancers. [Abstract]

2024 Dec 2;14(12):2430-2449. PMID: 39121480
Cancer Discov

D3S-001, a KRAS G12C inhibitor with rapid target engagement kinetics, overcomes nucleotide cycling and demonstrates robust preclinical and clinical activities. [Abstract]

2024 May 8. PMID: 38717075

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.
Nat Cancer

The MEK-RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers. [Abstract]

2026 Jan;7(1):116-130. PMID: 41482524
Nat Cancer

Co-targeting SOS1 enhances the antitumor effects of KRASG12C inhibitors by addressing intrinsic and acquired resistance. [Abstract]

2024 Sep;5(9):1352-1370. PMID: 39103541

Adagrasib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Sep;5(9):1352-1370. [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.
Nat Cancer

Scribble mis-localization induces adaptive resistance to KRAS G12C inhibitors through feedback activation of MAPK signaling mediated by YAP-induced MRAS. [Abstract]

2023 Jun;4(6):829-843. PMID: 37277529

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.
J Thorac Oncol

KRAS Secondary Mutations That Confer Acquired Resistance to KRAS G12C Inhibitors, Sotorasib and Adagrasib, and Overcoming Strategies: Insights From In Vitro Experiments. [Abstract]

2021 Aug;16(8):1321-1332. PMID: 33971321
Cancer Res

KRAS Inhibitor Induced Cancer Cell Death Enhances Sensitivity to Immune-Mediated Bystander Killing of Drug-Resistant Subclones. [Abstract]

2026 Jun 8. PMID: 42258763
Cancer Res

PRT3789 is a First-in-Human SMARCA2-Selective Degrader that Induces Synthetic Lethality in SMARCA4-Mutated Cancers. [Abstract]

2025 Sep 24. PMID: 40991405
Cancer Res

Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. [Abstract]

2025 Jan 2;85(1):101-117. PMID: 39437162
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Combining RAS(ON) G12C-selective inhibitor with SHP2 inhibition sensitises lung tumours to immune checkpoint blockade. [Abstract]

2024 Sep 25;15(1):8146. PMID: 39322643
Nat Commun

Signature-driven repurposing of Midostaurin for combination with MEK1/2 and KRASG12C inhibitors in lung cancer. [Abstract]

2023 Oct 10;14(1):6332. PMID: 37816716
J Clin Invest

Cotargeting DNA topoisomerase II enhances efficacy of RAS-targeted therapy in KRAS-mutant cancer models. [Abstract]

2026 Feb 16;136(4):e197192. PMID: 41697749
J Clin Invest

Co-targeting a MYC-eIF4A survival axis improves the efficacy of KRAS inhibitors in lung cancer. [Abstract]

2023 Aug 15;133(16):e167651. PMID: 37384411
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
J Exp Clin Cancer Res

Dual inhibition of HERs and PD-1 counteract resistance in KRASG12C-mutant head and neck cancer. [Abstract]

2024 Nov 20;43(1):308. PMID: 39567998
Sci Adv

Acquired resistance to KRAS G12C small-molecule inhibitors via genetic/nongenetic mechanisms in lung cancer. [Abstract]

2023 Oct 13;9(41):eade3816. PMID: 37831779
Redox Biol

Reactivation of MAPK-SOX2 pathway confers ferroptosis sensitivity in KRASG12C inhibitor resistant tumors. [Abstract]

2024 Nov 5:78:103419. PMID: 39527862
Clin Cancer Res

Overcoming Adaptive Resistance to KRASG12D Blockade in Pancreatic Cancer through Vertical Pathway Inhibition. [Abstract]

2026 Mar 9. PMID: 41801133
Cell Death Dis

Anlotinib enhances the efficacy of KRAS-G12C inhibitors through c-Myc/ORC2 axis inhibition in non-small cell lung cancer. [Abstract]

2025 May 2;16(1):356. PMID: 40316534
Cell Commun Signal

Adagrasib, a KRAS G12C inhibitor, reverses the multidrug resistance mediated by ABCB1 in vitro and in vivo. [Abstract]

2022 Sep 14;20(1):142. PMID: 36104708
Int J Biol Macromol

Ganoderma microsporum immunomodulatory protein combined with KRASG12C inhibitor impedes intracellular AKT/ERK network to suppress lung cancer cells with KRAS mutation. [Abstract]

2024 Feb;259(Pt 2):129291. PMID: 38211909
Acta Pharmacol Sin

143D, a novel selective KRASG12C inhibitor exhibits potent antitumor activity in preclinical models. [Abstract]

2023 Jul;44(7):1475-1486. PMID: 36725884
Cell Chem Biol

Systematic cysteine scanning identifies a druggable pocket in oncogenic KRAS. [Abstract]

2026 Feb 11:S2451-9456(26)00027-9. PMID: 41679298
Cell Rep

KRASG12C-independent feedback activation of wild-type RAS constrains KRASG12C inhibitor efficacy. [Abstract]

2022 Jun 21;39(12):110993. PMID: 35732135
Br J Cancer

Farnesyl-transferase inhibitors show synergistic anticancer effects in combination with novel KRAS-G12C inhibitors. [Abstract]

2024 Apr;130(6):1059-1072. PMID: 38278976
JCI Insight

YAP/TAZ mediates resistance to KRAS inhibitors through inhibiting proapoptosis and activating the SLC7A5/mTOR axis. [Abstract]

2024 Dec 20;9(24):e178535. PMID: 39704172
Clin Epigenetics

Selenite as a dual apoptotic and ferroptotic agent synergizes with EGFR and KRAS inhibitors with epigenetic interference. [Abstract]

2023 Mar 2;15(1):36. PMID: 36864513
ACS Omega

Application and Cross-Validation of a High-Throughput SPR Method for Characterizing Covalent Binding Ligands. [Abstract]

2025 Jul 4;10(27):29637-29646. PMID: 40687013
ACS Chem Biol

Repurposing the Damage Repair Protein Methyl Guanine Methyl Transferase as a Ligand Inducible Fusion Degron. [Abstract]

2022 Jan 21;17(1):24-31. PMID: 34982531
ACS Pharmacol Transl Sci

Suite of Biochemical and Cell-Based Assays for the Characterization of Kirsten Rat Sarcoma (KRAS) Inhibitors and Degraders. [Abstract]

2024 Dec 2;7(12):3921-3934. PMID: 39698278
Cancer Res Commun

Constitutive EGFR Activation Induced by PTPRR Downregulation Confers Resistance to KRAS Inhibitors. [Abstract]

2026 Mar 10. PMID: 41808249
Cancer Res Commun

The Selective WEE1 Inhibitor Azenosertib Shows Synergistic Antitumor Activity with KRASG12C Inhibitors in Preclinical Models. [Abstract]

2025 Feb 1;5(2):240-252. PMID: 39807828
FEBS Lett

LncRNA YIYA drives pancreatic cancer proliferation under high-glucose conditions by reinforcing a RAS-PKM2-dependent Warburg phenotype. [Abstract]

2026 Jun 8. PMID: 42253181
Technol Cancer Res Treat

VT204: A Potential Small Molecule Inhibitor Targeting KRASG12C Mutation for Therapeutic Intervention in Non-Small Cell Lung Cancer. [Abstract]

2024 Jan-Dec:23:15330338241264853. PMID: 39053018
J Chromatogr B Analyt Technol Biomed Life Sci

Validated extended multiplexed LC-MS/MS assay for the quantification of adagrasib and sotorasib in human plasma, together with four additional SMIs. [Abstract]

2023 Dec 1:1231:123918. PMID: 37979367
Biomed Chromatogr

Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]

2024 Oct;38(10):e5986. PMID: 39136165
bioRxiv

2026 Jun 19.
bioRxiv

2026 May 9.
bioRxiv

2026 Feb 20.
Weill Medical College of Cornell University

2025.
bioRxiv

2025 Nov 26.
bioRxiv

2025 Oct 28.
bioRxiv

2025 Oct 31.
bioRxiv

Genetic mechanisms of resistance to targeted KRAS inhibition. [Abstract]

2025 Aug 4:2025.08.04.668444. PMID: 40799582
bioRxiv

Post-Translational Modifications Remodel Proteome-Wide Ligandability. [Abstract]

2025 Aug 2:2025.07.31.667978. PMID: 40766426
Patent

US20250154156A1.
bioRxiv

2025 March 19.
bioRxiv

Revealing Functional Hotspots: Temperature-Dependent Crystallography of K-RAS Highlights Allosteric and Druggable Sites. [Abstract]

2025 Feb 28:2025.02.27.639303. PMID: 40060414
Patent

US20240238294A1
Patent

US20240238294A1.
bioRxiv

2024 July 23.
bioRxiv

2024 Jan 16.
bioRxiv

Oncogenic Kras G12D specific non-covalent inhibitor reprograms tumor microenvironment to prevent and reverse early pre-neoplastic pancreatic lesions and in combination with immunotherapy regresses advanced PDAC in a CD8 + T cells dependent manner. [Abstract]

2023 Feb 18:2023.02.15.528757. PMID: 36824971

Adagrasib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 18:2023.02.15.528757. [Abstract]

Adagrasib (MRTX849; 60 nM-1 µM) induces Fas expression in Kras^G12C mutant MIA PaCa-2 cells.
bioRxiv

Combined KRASG12C and SOS1 inhibition enhances and extends the anti-tumor response in KRASG12C-driven cancers by addressing intrinsic and acquired resistance. [Abstract]

2023 Jan 23:2023.01.23.525210. PMID: 36747713
Research Square Print

December 21st, 2022.
Journal of Pharmaceutical and Biopharmaceutical Research

2022 Jan 11.

Solvant et solubilité

In Vitro:

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)

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

1.6553 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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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: 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.

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:

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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:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[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]

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	1.6553 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

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Adagrasib

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