h2122

KRAS inhibitor-9 (DUN09716) 是一种 KRAS 抑制剂，阻止 GTP-KRAS 的形成和 KRAS 下游激活。它以中等的结合亲和力与 KRAS G12D、KRAS G12C 和 KRAS Q61H 蛋白结合，选择性抑制具有 KRAS 突变的 NSC-LC 细胞的增殖。它可导致 G2 M 细胞周期停滞并诱导凋亡。

SW209049 是一种硬脂酰辅酶A 9-去饱和酶抑制剂。 SW209049 对H2122细胞表现出有效的活性，IC50为0.13uM。

RBC8是一种特异性 GTP 酶 RalA RalB 抑制剂，通过抑制 Ral 与其效应物 RALBP1 的结合，对 GTP 酶 RhoA 和 Ras 没有抑制作用。

BQU57 能够选择性抑制 Ral，且对 Ral 的选择性高于 Ras、Rho，能够作用于 H2122(IC50:2.0 μM)和 H358(IC50:1.3 μM)。

SW203668 is an irreversible inhibitor of stearoyl-CoA desaturase (IC50 = 54 nM). It is selectively cytotoxic to H2122, H460, HCC44, and HCC95 cell lines that express cytochrome P450 (CYP) isoform CYP4F11 over eight other cancer cell lines that lack CYP4F11 in vitro (IC50s = 22-116 and >10,000 nM, respectively) and ectopic expression of CYP4F11 in SW203668-insensitive H1155 cells results in sensitization to SW203668. In vivo, SW203668 reduces tumor growth rate without reducing sebocyte production in the H2122 wild-type and nonobese diabetic severe combined immunodeficiency (NOD-SCID) mouse xenograft models when administered at doses of 20 and 6 mg kg, respectively.

G-573 is an allosteric inhibitor of MEK that is both potent and selective. The IC(50) value for pERK inhibition in HCT116 tumours by G-573 was estimated to be 0.406  µM. The IC(50) values for tumour growth inhibition in HCT116 and H2122 were estimated to be 3.43 and 2.56 µM, respectively. ED(50) estimates in HCT116 and H2122 mouse xenograft models were estimated to be ~4.6 and 1.9 mg kg day, respectively.