KRAS G12D inhibitor 14

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KRAS G12D inhibitor 14 是一种有效的 KRAS G12D 抑制剂，与 KRAS G12D蛋白结合的 KD 为 33 nM。KRAS G12D inhibitor 14 降低 KRAS G12D (KRAS G12D-GTP) 的活性形式，但不降低 KRAS G13D。

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.

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).

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.

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Others

Other Targets

Kras

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2765254-39-3

420.45

C20H19F3N4OS

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (118.92 mM; 超声助溶 (<60°C)

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

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(-20℃)

With Ice Pack

≥ 2 years