RMC-7977 | KRAS inhibitor

CAS:2765082-12-8

Catalog Number:10-3954

RMC-7977 (2765082-12-8) is broad spectrum inhibitor of both mutant and wild-type KRAS, NRAS, and 

HRAS variants.1 It binds with high affinity to cyclophilin A (KD = 195 nM) creating a binary complex that

has high affinity for the active state of KRAS (KD = 85 nM for G12V). Active in in vivo xenograft models 

of NSCLC, CRC, and PDAC.1,2,3 RMC-7977 was able to overcome resistance to the KRASG12D selective 

inhibitor MRTX1133.1

RMC-7977 (2765082-12-8)은 KRAS, NRAS, HRAS 변이의 돌연변이 및 원형 변이 모두에 대한 넓은 스펙트럼 

억제제입니다. 이는 cyclophilin A (KD = 195 nM)에 높은 치수로 결합하여 생성되는 이중 복합체를 생성하며, 

KRAS의 활성 상태 (KD = 85 nM for G12V)에 높은 치수로 결합합니다. RMC-7977은 NSCLC, CRC 및 PDAC의

 in vivo xenograft 모델에서 활성이 있습니다. RMC-7977은 KRASG12D 선택적 억제제 MRTX1133에 대한

 저항을 극복할 수 있습니다1.

CAS:2765082-12-8

Catalog Number:10-3954

Activity:KRAS inhibitor

Chemical Names:(1R,5S)-N-[(7S,13S)-20-[5-(4-cyclopropylpiperazin-1-yl)-2-[(1S)-1-methoxyethyl]pyridin-3-yl]

                           -21-ethyl-17,17-dimethyl-8,14-dioxo-15-oxa-4-thia-9,21,27,28-tetrazapentacyclo[17.5.2.12,5.

                            19,13.022,26]octacosa-1(25),2,5(28),19,22(26),23-hexaen-7-yl]-3-oxabicyclo[3.1.0]hexane-

                            6-carboxamide

Molecular Weight:865.11

Molecular Formula:C47H60N8O6S

Solubility:Soluble in DMSO (>75 mg/ml)

Physical Properties:Yellow solid

Purity:>98% HPLC

NMR: (Conforms)

Storage Temperature:-20°C

Stability:Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be

              stored at -20°C for up to 1 months.

Shipping Code:RT

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References/Citations:

1.Holderfield et al. (2024), Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy; Nature 629 919

2.Wasko et al. (2024), Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer; Nature 629 927

3.Araujo et al. (2024), Mechanisms of Response and Tolerance to Active RAS Inhibition in KRAS-Mutant Non-Small Cell 

Lung Cancer; Cancer Discov. 14 2183