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

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

KRAS G12D inhibitor 22 Chemical Structure

KRAS G12D inhibitor 22 Chemical Structure

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KRAS G12D inhibitor 22 Related Antibodies

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Description

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.

KRAS G12D inhibitor 22 Related Antibodies

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) 生物利用度 (%)
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.
Molecular Weight

644.66

Formula

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
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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KRAS G12D inhibitor 22 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:

KRAS G12D inhibitor 22RasASPC-1 cellsKRAS G12Dpancreatic cancerInhibitorinhibitorinhibit

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