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Calderasib (MK-1084) KRas inhibitor

Cat.No.E1829

Calderasib (MK-1084) is a selective KRAS G12C inhibitor demonstrating antitumor efficacy. It can be utilized as monotherapy or in combination with pembrolizumab () for oncology research.
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Quality Control

Batch: Purity: 98.17%
98.17

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (156.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 637.08 Formula

C32H31ClF2N6O4

Storage (From the date of receipt)
CAS No. 2641216-67-1 Download SDF Storage of Stock Solutions

Synonyms MK-1084 SMILES FC1=C2C(OCCOC3=CC=NC(C(C)C)=C3N4C5=NC2=C(Cl)C=C5C(N6[C@@H](C)CN(C(C=C)=O)[C@H](C)C6)=NC4=O)=C(F)C=C1

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Mechanism of Action

In vivo
Calderasib (MK-1084) (10-30 mg/kg, po for 14 days) exhibits antitumor efficacy in mouse MiaPaCa-2 xenograft models. This compound exhibits a good pharmacokinetic characteristics with a plasma clearance of 22 mL/min/kg, a mean residence time MRT of 1.1 h and an oral bioavailability of 61%.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-28)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07431827 RECRUITING
Non-small Cell Lung Cancer
Merck Sharp & Dohme LLC
2026-03-18 PHASE3
NCT07554339 RECRUITING
Non-small Cell Lung Cancer
Merck Sharp & Dohme LLC
2026-06-18 PHASE3
NCT07209111 RECRUITING
Neoplasm Malignant
Merck Sharp & Dohme LLC
2025-12-04 PHASE2
NCT05067283 RECRUITING
Advanced Solid Tumors
Merck Sharp & Dohme LLC
2021-12-17 PHASE1
NCT07190248 RECRUITING
Non-small Cell Lung Cancer
Merck Sharp & Dohme LLC
2025-10-08 PHASE3
NCT07252739 RECRUITING
Malignant Neoplasm
Merck Sharp & Dohme LLC
2025-12-19 PHASE2

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