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RMC-7977

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Purity:97.46%

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COA HPLC LCMS HNMR

RMC-7977

Catalog No. T81263Cas No. 2765082-12-8

RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.

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Pack Size	Price	Availability
1 mg	$263	In Stock
5 mg	$645	In Stock
10 mg	$987	In Stock
25 mg	$1,980	In Stock
50 mg	$3,290	In Stock
100 mg	$5,290	In Stock

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Product Introduction

Bioactivity

Description	RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.
In vitro	METHODS: U2OS cells were treated with 50 nM RMC-7977 to observe the formation of KRAS-CYPA complexes and disruption of KRAS(G12V)-CRAF interactions using a live-cell nano-bioluminescence resonance energy transfer (BRET) kinetic assay. RESULTS: RMC-7977 induced KRAS and CYPA binding and dissociated the CRAF RBD from KRAS at the same fast rate (signaling half-life (t1/2) < 5 min).[1] METHODS: RAS-dependent (KRAS, NRAS, or EGFR mutated) cancer cells treated with RMC-7977 (0.1,1,10,100,100 nM) were compared for activity of RMC-7977 in cancer cells harboring various activating mutations in the RAS pathway, specifically oncogenic variants of KRAS, NRAS, EGFR, or BRAF. RESULTS: Exhibited concentration-dependent inhibition of downstream signaling and proliferation in the low nanomolar range.[1]
In vivo	METHODS: U2OS cells were treated with 50 nM RMC-7977 to observe the formation of KRAS-CYPA complexes and disruption of KRAS(G12V)-CRAF interactions using a live-cell nano-bioluminescence resonance energy transfer (BRET) kinetic assay. RESULTS: RMC-7977 induced KRAS and CYPA binding and dissociated the CRAF RBD from KRAS at the same fast rate (signaling half-life (t1/2) < 5 min).[1] METHODS: RAS-dependent (KRAS, NRAS, or EGFR mutated) cancer cells treated with RMC-7977 (0.1,1,10,100,100 nM) were compared for activity of RMC-7977 in cancer cells harboring various activating mutations in the RAS pathway, specifically oncogenic variants of KRAS, NRAS, EGFR, or BRAF. RESULTS: Exhibited concentration-dependent inhibition of downstream signaling and proliferation in the low nanomolar range.[1]

Chemical Properties

Molecular Weight	865.09
Formula	C47H60N8O6S
Cas No.	2765082-12-8

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (115.59 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.1559 mL	5.7797 mL	11.5595 mL	57.7975 mL
5 mM	0.2312 mL	1.1559 mL	2.3119 mL	11.5595 mL
10 mM	0.1156 mL	0.5780 mL	1.1559 mL	5.7797 mL
20 mM	0.0578 mL	0.2890 mL	0.5780 mL	2.8899 mL
50 mM	0.0231 mL	0.1156 mL	0.2312 mL	1.1559 mL
100 mM	0.0116 mL	0.0578 mL	0.1156 mL	0.5780 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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RMC-7977

RMC-7977

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