MK-1084 free base · Synonyms: Calderasib

MK-1084 is a selective KRAS G12C inhibitor.

For research use only. Not for human or veterinary use.

Target Ras

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

MK-1084 structure

CAS No.: 2641216-67-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 mg	USD 850.00	BP-00334-1mg	In stock	Get quote
5 mg	USD 2,150.00	BP-00334-5mg	In stock	Get quote
10 mg	Inquire	BP-00334-10mg	In stock	Inquire

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Description

MK-1084 is a selective KRAS G12C inhibitor that is currently in Phase I clinical trial (NCT05067283). MK-1084 exhibits anticancer activity and can be used either alone or in combination with pembrolizumab for cancer research.

Biological activity

Calderasib (MK-1084) (0.01-10 μM, 2 h) inhibits the SOS-catalyzed nucleotide exchange with IC50 of 1.2 nM, inhibits the phosphorylation of ERK1/2 in cell H358 with IC50 of 9 nM

Specifications

MW (average): 637.0760
Formula: C₃₂H₃₁ClF₂N₆O₄
CAS No.: 2641216-67-1
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃, protect from light; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 100 mg/mL

Documents

References

[1]. Rojas C, et al. 663P Safety and preliminary efficacy of the KRAS G12C inhibitor MK-1084 in solid tumors and in combination with pembrolizumab in NSCLC[J]. Annals of Oncology, 2023, 34: S466-S467.

[2]. Ma X, et al., Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor. J Med Chem. 2024 Jul 11;67(13):11024-11052.

Same target

Search Ras

Same research area

Search Cancer