RMC-7977 | KRAS inhibitor

CAS:
 2765082-12-8
Catalog Number:
 10-3954
RMC-7977 chemical structure

Available Options

Size:PriceQuantity 
1 mg$80.00
5 mg$295.00

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

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
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

Safety Data Sheet:

Product Data Sheet:

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