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RMC-7977

🥰Excellent
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.

RMC-7977

RMC-7977

🥰Excellent
Purity: 98.20%
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.
Pack SizePriceAvailabilityQuantity
1 mg249 €In Stock
5 mg612 €In Stock
10 mg937 €In Stock
25 mg1.881 €In Stock
50 mg3.125 €In Stock
100 mg5.025 €In Stock
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Purity:98.20%
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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 Weight865.09
FormulaC47H60N8O6S
Cas No.2765082-12-8
SmilesO=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
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (115.59 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.1559 mL5.7797 mL11.5595 mL57.7975 mL
5 mM0.2312 mL1.1559 mL2.3119 mL11.5595 mL
10 mM0.1156 mL0.5780 mL1.1559 mL5.7797 mL
20 mM0.0578 mL0.2890 mL0.5780 mL2.8899 mL
50 mM0.0231 mL0.1156 mL0.2312 mL1.1559 mL
100 mM0.0116 mL0.0578 mL0.1156 mL0.5780 mL

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