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

KRASG12C IN-2 (compound 17) is an orally active KRASG12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice.

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KRASG12C IN-2 Chemical Structure

KRASG12C IN-2 Chemical Structure

CAS No. : 2706637-12-7

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KRASG12C IN-2 Related Antibodies

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Description

KRASG12C IN-2 (compound 17) is an orally active KRASG12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice[1].

IC50 & Target

KRASG12C[1].
In Vitro

KRASG12C IN-2 (0-100 nM; 72 h) inhibits the inhibition of the proliferation of KRASG12C mutant MIA-PA-CA-2 cells, with an IC50 value of 0.44 nM[1].

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

KRASG12C IN-2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MIA-PA-CA-2 cells (with KRASG12C mutant)
Concentration: 0-100 nM
Incubation Time: 72 h
Result: Exhibited antiproliferation activity (IC50 = 0.44 nM).
In Vivo

KRASG12C IN-2 (10, 30 mg/kg; p.o.; single daily for 22 days) inhibits tumor growth in mice[1].

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

Animal Model: Nude Balb/c mice (Subcutaneous transplantation model of Mia PaCa-2 cells)[1].
Dosage: 10, 30 mg/kg
Administration: Oral administration; single daily for 22 days.
Result: Inhibited tumor growth in mice, and the inhibition rates are 93.06% (dosage at 10 mg/kg) and 99.64% (dosage at 30 mg/kg), respectively.
Animal Model: Male SD rats and male CD mice[1].
Dosage: 2.0 mg/kg
Administration: i.v.; single
Result: 1.19 Pharmacokinetic Parameters of KRASG12C IN-2 in Male SD rats and Male CD mice[1].
Male SD rats Male CD mice
IV (2 mg/kg) IV (2 mg/kg)
T1/2 (h) 1.9 1.7
CL (mL/min/kg) 71.5 40.6
Vdss/Vdss, u(L/kg) 10.6/221 3.9/32.3
AUC0-last/AUCu (nM•h) 653/31.3 1297/155.6
Animal Model: Male SD rats and male CD mice[1].
Dosage: 9.8, 10.3 mg/kg
Administration: p.o.; single
Result: 1.19 Pharmacokinetic Parameters of KRASG12C IN-2 in Male SD rats and Male CD mice[1].
Male SD rats Male CD mice
PO (9.8 mg/kg) PO (10.3 mg/kg)
AUC0-last/AUCu (nM•h) 995/47.8 1422/170.6
Tmax (h) 1.5 1.0
Cmax/Cmax, u (nM) 220/10.6 431/51.7
F (%) 30.5% 21.9%
Molecular Weight

679.66

Formula

C32H35F6N7O3
CAS No.
SMILES

FC(F)(F)C(C(C)=CC(N)=C1F)=C1[C@H]2CC3=NC(OC[C@@]45N(CCC5)C[C@@H](C4)F)=NC(N6C[C@@H](N(CC6)C(C(F)=C)=O)CC#N)=C3CO2
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
References
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KRASG12C IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KRASG12C IN-22706637-12-7RasMIA-PA-CA-2 cellscancerInhibitorinhibitorinhibit

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