2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt
  3. Ras ERK
  4. KRASG12D-IN-8

KRASG12D-IN-8 is an orally active KRASG12D inhibitor, with a Kd value of 0.003 nM for KRASG12D and 0.024 nM for KRASG12V. 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.

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

KRASG12D-IN-8

KRASG12D-IN-8 Chemical Structure

CAS No. : 3101973-42-3

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KRASG12D-IN-8 Related Antibodies

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Description

KRASG12D-IN-8 is an orally active KRASG12D inhibitor, with a Kd value of 0.003 nM for KRASG12D and 0.024 nM for KRASG12V. 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[1].

IC50 & Target[1]

KRas G12D

0.003 nM (Ki)

KRas G12V

0.024 nM (Ki)

In Vitro

KRASG12D-IN-8 (Compound 12) binds to KRASG12D with a Kd of 0.003 nM and to KRASG12V with a Kd 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.

KRASG12D-IN-8 Related Antibodies
Parmacokinetics
Species Dose Route CL Vdss 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].
Molecular Weight

662.70

Formula

C35H37F3N6O4
CAS No.
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
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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KRASG12D-IN-8 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:

KRASG12D-IN-83101973-42-3RasERKExtracellular signal regulated kinasesSwitch-II pocketGDP-bound KRASG12DGDP-bound KRASG12VKRAS mutant cancer cellsKRASG12Dmouse xenograft modelsRKN cellsKRASG12Vphospho-ERKMDCK cellsInhibitorinhibitorinhibit

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