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Cat. No.: HY-151999

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KRAS G12C inhibitor 65

KRAS G12C inhibitor 65 is a potent and covalent KRAS^G12C inhibitor that traps KRAS^G12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer.

For research use only. We do not sell to patients.

CAS No.: 3033305-77-7
Formula: C₁₉H₁₈Cl₂FN₃O₂
Molecular Weight:410.27

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

KRAS G12C inhibitor 65 Chemical Structure

CAS No.: 3033305-77-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Ras Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	9.3 μM Compound: 20a	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36228411]
MRC5	IC₅₀	6.1 μM Compound: 20a	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36228411]
NCI-H2228	IC₅₀	11.6 μM Compound: 20a	Antiproliferative activity against human NCI-H2228 cells harboring wild type KRAS assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells harboring wild type KRAS assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36228411]
NCI-H23	IC₅₀	1.3 μM Compound: 20a	Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36228411]
NCI-H358	IC₅₀	0.5 μM Compound: 20a	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36228411]
NCI-H441	IC₅₀	4.4 μM Compound: 20a	Antiproliferative activity against human NCI-H441 cells harboring KRAS G12V mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H441 cells harboring KRAS G12V mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36228411]
SK-LU-1	IC₅₀	4.6 μM Compound: 20a	Antiproliferative activity against human SK-LU-1 cells harboring KRAS G12D mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-LU-1 cells harboring KRAS G12D mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36228411]

In Vitro

KRAS G12C inhibitor 65 (compound 20a) (72 h) shows potent and selective antiproliferative activities against KRAS^G12C NSCLC cells, with IC₅₀s of 0.5 μM against NCI-H358 cells and 1.30 μM against NCI-H23 cells, with 7- to 21-fold selectivity over KRAS^G12S and KRAS^WT cells^[1].
KRAS G12C inhibitor 65 (0.5-8.0 μM; 6 h) decreases the phosphorylation of ERK and AKT in KRAS^G12C-mutant NCIH358 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

NCI-H358 and NCI-H2228 cells
Concentration:

0.5, 1.0, 2.0, 4.0, 8.0 μM
Incubation Time:

6 hours
Result:

Showed no impact on KRAS signaling in KRAS^WT NCI-H2228 cells.
The pERK level decreased 40%-90%, and the pAKT level was down-regulated by 30%-90% in NCI-H358 cells.

In Vivo

KRAS G12C inhibitor 65 (compound 20a) (10-15 mg/kg; i.p. every 2 d for 21 d) inhibited tumor growth in H358 xenografts by suppressing KRAS^G12C signalling^[1].

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

Animal Model:

Female BALB/c Nude mice were injected subcutaneously with NCI-H358 cells^[1]
Dosage:

10, 15 mg/kg
Administration:

I.p. every two days for 21 days
Result:

Significantly inhibited tumor growth while the body weight of mice was not influenced.

Chemical Information

CAS No. 3033305-77-7
Molecular Weight 410.27
Formula C₁₉H₁₈Cl₂FN₃O₂
SMILES

O=C(N1CCN(CC1)C(NC2=CC(C3=C(C=CC=C3)F)=C(C=C2)Cl)=O)CCl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cheng R, et, al. Design, synthesis, and evaluation of 4(1H)-quinolinone and urea derivatives as KRASG12C inhibitors with potent antitumor activity against KRAS-mutant non-small cell lung cancer. Eur J Med Chem. 2022 Dec 15;244:114808. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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KRAS G12C inhibitor 65

All Ras Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

KRAS G12C inhibitor 65 Related Classifications

HY-151999 Related Classifications