2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRASG12C IN-17

KRASG12C IN-17 is an orally active covalent KRASG12C inhibitor, showing strong inhibitory activity in KRASG12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRASG12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer.

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KRASG12C IN-17

KRASG12C IN-17 構造式

CAS 番号 : 2966924-23-0

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KRASG12C IN-17 関連抗体

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製品説明

KRASG12C IN-17 is an orally active covalent KRASG12C inhibitor, showing strong inhibitory activity in KRASG12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRASG12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer[1].

IC50 & Target

KRas G12C

 

体外実験

KRASG12C IN-17 (compound 19) potently inhibits KRASG12C-mutant NCI-H23 and NCI-H358 cells with IC50 values of 0.7 nM and 0.5 nM, respectively , following 72-144 hours of incubation[1].
KRASG12C IN-17 covalently modifies KRASG12C in both GDP- and GMPPNP-bound states with >96% conjugation efficiency within 15 minutes[1].
KRASG12C IN-17 inhibits multiple resistance-associated KRASG12C variants, including R68S, H95Q, Y96C and Q99L, in Ba/F3 cells[1].
KRASG12C IN-17 exhibits antiproliferative activity against selected KRASG12C secondary-mutation cancer cell lines, retaining strong potency particularly against Y96C and Q99L variants[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KRASG12C IN-17 関連抗体

Cell Proliferation Assay[1]

Cell Line: NCI-H23 (KRASG12C), NCI-H358 (KRASG12C)
Concentration: 0.7 nM (NCI-H23), 0.5 nM (NCI-H358)
Incubation Time: 72 h
Result: Significantly inhibited proliferation of KRASG12C-mutant NCI-H23 and NCI-H358 cells.
体内実験

KRASG12C IN-17 (30 mg/kg, oral gavage, QD for 28 days) demonstrates strong in vivo activity, producing 103% tumor growth inhibition in SW837 KRASG12C xenograft models[1].
KRASG12C IN-17 (30 mg/kg, oral gavage, QD for 21 days) significantly reduces tumor volume in Ba/F3 KRASG12C/R68S xenograft models, achieving 65.9% tumor reduction[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SW837 human rectal cancer xenograft (KRASG12C) female NOD SCID mice (6–7 weeks old, 20.5–23.7 g)
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily (QD); 28 days
Result: Achieved 103% tumor growth inhibition and induced near-complete tumor stasis without significant body-weight loss in SW837 KRASG12C xenograft models.
Animal Model: Ba/F3 KRASG12C/R68S xenograft model female NOD SCID mice (6-8 weeks old, 18.6-23.3 g)
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily (QD); 21 days
Result: Reduced tumor volume by 65.9% and demonstrated good tolerability in Ba/F3 KRASG12C/R68S xenograft models.
分子量

650.69

分子式

C37H33F3N6O2
CAS 番号
SMILES

N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C=C(F)C(C4=C5C(C#C)=CC=CC5=CC=C4)=C(F)C3=NC(OCC67CCCN6CCC7)=N2)C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
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KRASG12C IN-17 Related Classifications

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Keywords:

KRASG12C IN-172966924-23-0RasKRAS G12Ccovalent inhibitorcolorectal cancerNSCLCresistance mutationR68Sxenograftoral bioavailabilitytumor stasisInhibitorinhibitorinhibit

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