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Chemical Structure| 2765082-12-8 Chemical Structure| 2765082-12-8

Structure of RMC-7977
CAS No.: 2765082-12-8

Chemical Structure| 2765082-12-8

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RMC-7977 is a broad-spectrum tri-complex RAS inhibitor capable of inhibiting both mutant and wild-type KRAS, NRAS, and HRAS, especially showing significant antitumor activity in RAS-dependent tumors, suitable for RAS-driven cancer research. This compound demonstrates good tolerability and anticancer effects in various preclinical cancer models.

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of RMC-7977

CAS No. :2765082-12-8
Formula : C47H60N8O6S
M.W : 865.09
SMILES Code : O=C1OCC(C)(C)CC=2C3=CC(=CC=C3N(C2C=4C=C(C=NC4C(OC)C)N5CCN(CC5)C6CC6)CC)C=7N=C(SC7)CC(NC(=O)C8C9COCC89)C(=O)N%10NC1CCC%10
English Name :(1α,5α,6α)-N-[(2R,14S,18S)-2-[5-(4-Cyclopropyl-1-piperazinyl)-2-[(1S)-1-methoxyethyl]-3-pyridinyl]-1-ethyl-18,19,20,21-tetrahydro-25,25-dimethyl-15,22-dioxo-17H-5,3-([4,2]-endo-thiazolopropano[1,3]-endo-pyridazinomethanoxypropano)-1H-indol-14-yl]-3-oxabicyclo[3.1.0]hexane-6-carboxamide
MDL No. :N/A

Safety of RMC-7977

Related Pathways of RMC-7977

epigenetics
DNA
GPCR
MAPK
PI3K-AKT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
AsPC-1 cells 2.20 nM 120 hours Evaluate the inhibitory effect of RMC-7977 on proliferation of KRASG12D mutant cells, EC50 of 2.20 nM Nature. 2024 May;629(8013):919-926
NCI-H441 cells 2.40 nM 120 hours Evaluate the inhibitory effect of RMC-7977 on proliferation of KRASG12V mutant cells, median EC50 of 2.40 nM Nature. 2024 May;629(8013):919-926
Capan-1 cells 965 nM 120 hours Evaluate the inhibitory effect of RMC-7977 on proliferation of KRASG12V mutant cells, EC50 of 965 nM Nature. 2024 May;629(8013):919-926
HPAC cells 100 nM 24 hours Assessed the effect of RMC-7977 on phosphorylation of RAS-RAF effector proteins ERK1/2 in HPAC cells, showing reduced phosphorylation of ERK1/2. Nature. 2024 May;629(8013):927-936

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Human PDAC cell line-derived xenograft (CDX) and patient-derived xenograft (PDX) models Orally 10 mg/kg Daily for 21–28 days Assessed the anti-tumor activity of RMC-7977 in xenograft models, showing significant anti-tumor activity in all 10 models, with tumor regressions observed in 7 models. Nature. 2024 May;629(8013):927-936
BALB/c nude mice NCI-H441 CDX model Oral 10 mg/kg Once daily for 28 days Evaluate the anti-tumor effect of RMC-7977 in KRASG12V mutant tumor model, resulting in 83% mean tumor regression Nature. 2024 May;629(8013):919-926

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.16mL

0.23mL

0.12mL

5.78mL

1.16mL

0.58mL

11.56mL

2.31mL

1.16mL

References

 

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