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Art. -Nr.: HY-184010

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KRASG12D-IN-8

KRASG12D-IN-8 is an orally active KRAS^G12D inhibitor, with a K_d value of 0.003 nM for KRAS^G12D and 0.024 nM for KRAS^G12V. KRASG12D-IN-8 inhibits the activity of phosphorylated ERK in KRAS-mutated cells. KRASG12D-IN-8 induces tumor regression in ovarian cancer xenograft mouse models. KRASG12D-IN-8 can be used for the research of KRAS-mutated cancers.

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CAS. Nr.: 3101973-42-3
Formel: C₃₅H₃₇F₃N₆O₄
Molecular Weight:662.70

Speicherung:

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

KRASG12D-IN-8 Chemical Structure

CAS. Nr.: 3101973-42-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

KRas G12D

0.003 nM (Ki)

KRas G12V

0.024 nM (Ki)

Alle Ras Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

In Vitro

KRASG12D-IN-8 (Compound 12) binds to KRAS^G12D with a K_d of 0.003 nM and to KRAS^G12V with a K_d of 0.024 nM, exhibiting exceptional high-affinity interactions with both mutant KRAS proteins^[1].
KRASG12D-IN-8 has a low efflux permeability of 15.4 ×10⁻⁶ cm/s in MDCK cells, with intrinsic clearance values of 338 μL/min/mg in human liver microsomes and 542 μL/min/mg in mouse liver microsomes^[1].

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

Parmacokinetics

Species	Dose	Route	CL	V_dss	Bioavailability	AUC
Mice^[1]	10 mg/kg	p.o.	19.2 mL/min/kg	1.98 L/kg	13 %	2950
Rat^[1]	3 mg/kg	p.o.	61.7 mL/min/kg	4.46 L/kg	0.3 %	/
Dog^[1]	1 mg/kg	p.o.	8.5 mL/min/kg	6.99 L/kg	8.7 %	/

In Vivo

KRASG12D-IN-8 (0.3-3 mg/kg; p.o.; once daily; 2 weeks) exhibits anti-tumor activity in a RKN xenograft mouse model^[1].

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

Animal Model:

RKN tumor bearing SCID-Beige mice^[1]
Dosage:

0.3-3 mg/kg
Administration:

p.o.; once daily; 2 weeks
Result:

Inhibited RKN tumor growth in a dose-dependent manner, with tumor inhibition of 38.8%, tumor
regression of -45.2% and -89.4% across 0.3, 1 and 3 mpk dose, respectively.
Were well tolerated without body weight loss^[1].

Chemical Information

CAS. Nr. 3101973-42-3
Molecular Weight 662.70
Formel C₃₅H₃₇F₃N₆O₄
SMILES

C[C@@]12CCCN(C3=NC(OC[C@@]45CCCN4C[C@@H](C5)F)=NC6=C(C(C7=CC(O)=CC8=CC=C(C(CCCOC(N2)=O)=C78)F)=NC=C36)F)C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Phillips DP, et al. Targeting Multiple KRAS Mutations with High-Affinity Macrocyclic Inhibitors: From Discovery to Preclinical Validation. J Med Chem. Published online May 19, 2026. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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KRASG12D-IN-8

Alle Ras Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen