1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. KRAS G12D inhibitor 22

KRAS G12D inhibitor 22 (compound 6) is a inhibitor of KRAS mutation. KRAS G12D inhibitor 22 has high activity (IC50<100 nM), good selectivity and low toxicity.KRAS G12D inhibitor 22 can be used in breast cancer research.

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KRAS G12D inhibitor 22

KRAS G12D inhibitor 22 화학구조

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제품 설명

KRAS G12D inhibitor 22 (compound 6) is a inhibitor of KRAS mutation. KRAS G12D inhibitor 22 has high activity (IC50<100 nM), good selectivity and low toxicity.KRAS G12D inhibitor 22 can be used in breast cancer research[1].

IC50 & Target[1]

KRas G12D

<100 nM (IC50)

In Vitro

KRAS G12D inhibitor 22 (0.08-20 μM; 72 h) has a good inhibitory effect on the growth of AGS cells (IC50<500 nM)[1].
KRAS G12D inhibitor 22 shows high inhibitory effect on KRAS G12D protein (IC50<100 nM)[1].
KRAS G12D inhibitor 22 (0.08-20 μM; 72 h) has batter anti-proliferation activity of ASPC-1 and AGS cells than that of MRTX1133 (HY-134813), and has better selection effect to other Kras G12C mutant cell lines[1].

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

Cell Proliferation Assay[1]

Cell Line: AGS, AsPC-K, NCI-H358, MOLM13 cells
Concentration: 0.08-20 μM
Incubation Time: 72 h
Result: Had good inhibitory effect on the growth of Kras, Gl2D mutant AGS, ASPC-1 cells.
Had weak inhibitory effect on the growth of KRASG12C-mutated cell line NCI-H358 and Kras wild-type cell line MOLMl3.
In Vivo

KRAS G12D inhibitor 22 (3 and 5 mg/kg; i.v. and i.p.; 0-24 h) can reach the effective concentration of inhibiting tumor cell growth after a single administration, and has good bioavailability in Male SD rat[1].
Pharmacokinetic Analysis in Male SD ratl[1]

Route Dose (mg/kg) T1/2 (h) Cmax (ng/mL) Tmax (h) CL (mL/min/kg) Vss (L/kg) AUG0_t (ng/mL h) Bioavailability (%)
i.v. 5 0.63 2163 0.08 96.4 3.5 1128 /
i.p. 3 1.03 177 0.25 / / 255.8 37.79

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

Animal Model: Male SD rat[1]
Dosage: 3 and 5 mg/kg
Administration: i.v. and i.p.
Result: Reached the effective concentration of inhibiting tumor cell growth after a single administration, and has good bioavailability.
분자량

644.66

화학식

C35H32F4N6O2

SMILES

OC1=CC(C=CC(F)=C2C#C)=C2C(C3=NC=C4C(N=C(OCC5(CCC6)N6CC7(C(F)(F)C7)C5)N=C4N8C[C@H]9N[C@H](CC9)C8)=C3F)=C1

선적

Room temperature in continental US; may vary elsewhere.

보관

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

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상품명:
KRAS G12D inhibitor 22
Cat. No.:
HY-162444
수량:
MCE Japan Authorized Agent: