2. GPCR/G Protein MAPK/ERK Pathway PI3K/Akt/mTOR Stem Cell/Wnt
  3. Ras Akt Raf ERK
  4. KRAS-IN-58

KRAS-IN-58 is a KRAS inhibitor with a IC50 of 0.223 μM against KRASG12D. KRAS-IN-58 binds to KRASG12C and KRASG12D proteins, and reduces the levels of phosphorylated Raf1, AKT and ERK in pancreatic cancer cells. KRAS-IN-58 can be used for the research of pancreatic cancer.

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

KRAS-IN-58

KRAS-IN-58 Chemical Structure

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KRAS-IN-58 Related Antibodies

Top Publications Citing Use of Products

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K-Ras H-Ras N-Ras Ras

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Akt Akt1 Akt2 Akt3

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B-Raf C-Raf Raf

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ERK ERK1 ERK2 ERK5 ERK8

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Description

KRAS-IN-58 is a KRAS inhibitor with a IC50 of 0.223 μM against KRASG12D. KRAS-IN-58 binds to KRASG12C and KRASG12D proteins, and reduces the levels of phosphorylated Raf1, AKT and ERK in pancreatic cancer cells. KRAS-IN-58 can be used for the research of pancreatic cancer[1].

IC50 & Target[1]

KRas G12D

223 nM (IC50)

In Vitro

KRAS-IN-58 (Compound 10b) (24 h) inhibits viability of ASPC-1, PANC-1, and Miapac-2 pancreatic cancer cells with IC50 values of 1.16 μM, 6.59 μM, and 6.432 μM, respectively[1].
KRAS-IN-58 (24 h) inhibits viability of SW1990 pancreatic cancer cells with an IC50 of 1.518 μM, while showing much weaker activity against LO2 normal hepatic cells (IC50 = 55.53 μM) and HPDE6-C7 normal pancreatic epithelial cells (IC50 = 10.50 μM), demonstrating selective activity for cancerous over non-cancerous cells[1].
pan-KRAS-IN-19 (1.25-20 μM) dose-dependently downregulates levels of KRAS, pRaf1, pAKT, and pERK in ASPC-1 and Miapac-2 pancreatic cancer cells[1].

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

KRAS-IN-58 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax MRT CL Vss Vz AUC
Mice[1] 2 mg/kg i.v. 4.3 h / / 0.512 h 66 mL/min/kg 2.6 L/kg 26 L/kg 510 ng·h/mL
Mice[1] 10 mg/kg p.o. 6.52 h 0.333 h 1.4 ng/mL 2.82 h / / / /
Molecular Weight

451.52

Formula

C21H17N5O3S2
SMILES

CN1C=CC=C1/C=C2SC(N(C\2=O)CCSC3=NN=C(O3)C4=CNC5=C4C=CC=C5)=O
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-IN-58 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-IN-58RasAktRafERKPKBProtein kinase BRaf kinasesExtracellular signal regulated kinasespAKTSW1990KRASG12CASPC-1KRASG12DpERKpRaf1Miapac-2pancreatic cancer cellsPANC-1Inhibitorinhibitorinhibit

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