ret v804m

AD80 是多激酶抑制剂，可抑制 RET、RAF、SRC 和 S6K，并大大降低 mTOR 活性。

RET V804M-IN-1 (RETV804M kinase inhibitor) 是一种 wt-RET 选择性的RETV804M 激酶抑制剂，其IC50=20 nM。

RET-IN-1 is a RET kinase inhibitor (IC50s: 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively).

Selpercatinib (LOXO-292) 是 RET 激酶抑制剂，抑制 RET (WT)、RET (V804M) 、RET (G810R)的 IC50分别为 14.0 nM、24.1 nM、530.7 nM，具有抗肿瘤活性。

RET-IN-23 是一种可口服且具有高效性的 RET 抑制剂，具有显著的抗肿瘤活性，可用于研究非小细胞肺癌。

Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase. It demonstrates nanomolar potency against RET while exhibiting over 300-fold selectivity against VEGFR2. Zeteletinib exhibits remarkable efficacy against the wild-type RET, RET V804M L gatekeeper mutants, as well as the frequently occurring oncogenic RET mutation M918T. Its antitumor activity is potent.

RET-IN-14 是 RET 的有效抑制剂，能够作用于 RET (WT) (IC50<0.51 nM)、RET (G810R) (IC50: 9.3 nM)、RET (V804M) (IC50: 1.3 nM)、BTK (C481S) (IC50: 9.2 nM) 和 BTK (C481S) (IC50: 15 nM)。RET-IN-14 表现出潜力进行肿瘤的研究。

RET-IN-12 是一种 RET 抑制剂，能够作用于 RET(WT) (IC50: 0.3 nM) 和 RET(V804M) (IC50: 1 nM)。

RET-IN-19 是 RET 的有效抑制剂，能够作用于 RET-wt (IC50: 6.8 nM) 和 RET V804M (IC50: 13.51 nM)，表现出抗癌效果。RET-IN-19 能够用于研究非小细胞肺癌 (NSCLC)。

Pralsetinib (Blu667) 是高效的、选择性的RET 抑制剂。它能够抑制 WT RET (IC50:0.4 nM)，RET 突变体 V804L (IC50:0.3 nM)，V804M (IC50:0.4 nM)，M918T (IC50:0.4 nM) 和 CCDC6-RET (IC50:0.4 nM) 的融合。

RET-IN-13 是一种喹啉化合物，一种有效的 RET 抑制剂，对 RET(WT) 和 RET(V804M) 的 IC50分别为 0.5 nM 和 0.9 nM。RET-IN-13 具有用于与RET 异常激活相关的肿瘤或肠道疾病研究的潜力。

RET-IN-16 是一种有效且具有选择性的RET 抑制剂，对RET(WT)，RET(M918T)，RET(V804L)，RET(V804M)，RET-CCDC6和RET-KIF5B 的IC50分别为 3.98 nM，8.42 nM，15.05 nM，7.86 nM，5.43 nM 和 8.86 nM。RET-IN-16 具有抗癌作用。

QZ2135 (compound 20) 是一种针对RET的PROTAC降解剂，并在Ba F3-KIF5B-RET-G810C异种移植小鼠模型中展示了抗肿瘤特性。QZ2135对于KIF5B-RET的降解活性DC50为4.7 nM (WT)、17.2 nM (V804M)、73.8 nM (G810C)。该化合物由靶蛋白配体 (red part)RETligand-3、E3连接酶配体 (blue part)Lenalidomide-F和PROTAC Linker (black part)7-Iodohept-1-yne组成，其中靶蛋白配体和linker形成偶联物RETLigand-Linker Conjugate-1。

Pralsetinib is a selective and next-generation RET inhibitor (IC50: 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T, and CCDC6-RET fusion). BLU-667 is an effective and selective inhibitor of RET mutations, fusions, and predicted resistant mutants.

RET-IN-22（compound 17b）是一种有效且选择性的口服活性RET抑制剂，其对野生型RET和RET-V804M的IC50分别为20.9 nM与18.3 nM。该化合物展现出对多数激酶，特别是EGFR和VEGFR2的高度选择性，表现出抗癌活性。

RET-IN-4 is a highly effective and specific RET inhibitor that can be administered orally. It demonstrates remarkable potency, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM for inhibiting RET variants including RET (WT), RET (V804M), and RET (M918T), respectively. Moreover, RET-IN-4 exhibits superior selectivity towards kinases JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). Additionally, RET-IN-4 possesses pronounced anticancer properties.

Zeteletinib hemiadipate (BOS-172738; DS-5010) is an orally active compound that functions as a selective inhibitor of RET kinase. It exhibits nanomolar potency against RET and a 300-fold selectivity towards VEGFR2. Notably, Zeteletinib hemiadipate demonstrates exceptional effectiveness against various forms of RET, including the wild type, RET V804M L gatekeeper mutants, and the oncogenic RET mutation M918T. Additionally, Zeteletinib hemiadipate exerts potent antitumor effects.

RET-IN-28 (Compound 16) 是一种 RET (跨膜受体酪氨酸蛋白激酶) 抑制剂，能够抑制突变型 RET 酶 (RET-V804M) 的活性，适用于癌症研究。