KRAS G12D inhibitor 14( —— )

Catalog No. M35624 CAS No. 2765254-39-3

KRAS G12D inhibitor 14 is a potent compound that binds the KRAS G12D protein (Kd: 33 nM) and selectively inhibits the active form KRAS G12D-GTP, but not KRAS G13D.

Purity : >98% (HPLC)

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Datasheet

HNMR

HPLC

MSDS

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Biological Information

Product Name

KRAS G12D inhibitor 14
Note

Research use only, not for human use.
Brief Description

KRAS G12D inhibitor 14 is a potent compound that binds the KRAS G12D protein (Kd: 33 nM) and selectively inhibits the active form KRAS G12D-GTP, but not KRAS G13D.
Description

KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D.
In Vitro

KRAS G12D inhibitor 14 (compound KD-8) shows antiproliferative activity with an IC50 of 2.1 μM against three KRAS G12D-mutated cells (Panc1, SW1990 and CT26). KRAS G12D inhibitor 14 decreases the active form of KRAS (KRAS-GTP) in KRAS G12D mutated cancer cell lines (CT26 and SW1990) but not in KRAS G13D mutated cancer cell lines (HCT116). KD-8 also causes efficient apoptosis of SW1990 and CT26 cancer cells. KRAS G12D inhibitor 14 down-regulates the phosphorylated Raf and Erk in CT26 and SW1990 cancer cell lines but not in HeLa cells (KRAS WT).
In Vivo

KRAS G12D inhibitor 14 (compound KD-8) (40 mg/kg or 60 mg/kg; i.p.) exhibits significant antitumor efficacy in a CT26 tumor model with a tumor growth inhibition (TGI) of 42% or 53% without causing apparent toxicity.
Synonyms

——
Pathway

Others
Target

Other Targets
Recptor

Kras
Research Area

——
Indication

——

Chemical Information

CAS Number

2765254-39-3
Formula Weight

420.45
Molecular Formula

C20H19F3N4OS
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 50 mg/mL (118.92 mM; Ultrasonic (<60°C)
SMILES

O(C)C1=C(C2=CC3=C(N=CN=C3S2)N4C5CCC(C4)NC5)C=C(C(F)(F)F)C=C1
Chemical Name

——

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. Li L, et al. Discovery of Thieno[2,3-d]pyrimidine-based KRAS G12D inhibitors as potential anticancer agents via combinatorial virtual screening. Eur J Med Chem. 2022;233:114243.?

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