KRASG12C IN-2

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KRASG12C IN-2 (compound 17) is an orally active KRAS^G12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice.

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

KRASG12C IN-2 Chemical Structure

CAS No. : 2706637-12-7

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Other Forms of KRASG12C IN-2:

D3S-001 Get quote
KRAS G12C inhibitor 59 Get quote

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References
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Description

KRASG12C IN-2 (compound 17) is an orally active KRAS^G12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice^[1].

IC₅₀ & Target

KRAS^G12C^[1].

In Vitro

KRASG12C IN-2 (0-100 nM; 72 h) inhibits the inhibition of the proliferation of KRAS^G12C 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.

Cell Proliferation Assay^[1]

Cell Line:	MIA-PA-CA-2 cells (with KRAS^G12C 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)
T_1/2 (h)	1.9	1.7
CL (mL/min/kg)	71.5	40.6
Vd_ss/Vd_ss, u(L/kg)	10.6/221	3.9/32.3
AUC_0-last/AUC_u (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)
AUC_0-last/AUC_u (nM•h)	995/47.8	1422/170.6
T_max (h)	1.5	1.0
C_max/C_{max, u} (nM)	220/10.6	431/51.7
F (%)	30.5%	21.9%

Molecular Weight

679.66

Formula

C₃₂H₃₅F₆N₇O₃

CAS No.

2706637-12-7

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

Handling Instructions (2659 KB)

References

[1]. Zhang Yang, et al. Pyrimidoheterocyclic compounds and application thereof. WO2021180181A1.

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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