C语言中ret的作用,c-RET抑制剂 | c-RET Inhibitor

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S1178

Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 是一个多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR-β，Kit (c-Kit)，RET (c-RET)和Raf-1，在无细胞试验中IC50分别是13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM和2.5 nM。Regorafenib 可诱导自噬。

Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05

S2736

Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3) 和 Ret (c-RET)，对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。

Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.

S1107

Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C，无细胞试验中IC50为13 nM/79 nM/61 nM，适度有效作用于Abl，TrkA，c-RET和FGFR1，对Lck，VEGFR2/3，c-Kit，CDK2等作用效果稍弱。Danusertib 可诱导凋亡、细胞周期阻滞和自噬。Phase 2。

Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).

S1244

Amuvatinib (MP-470, HPK 56) 是一种有效的，作用于c-Kit、PDGFα和Flt3的多靶点抑制剂，IC50分别为10 nM、40 nM和81 nM。Amuvatinib 可抑制c-MET和c-RET。Amuvatinib 还具有DNA修复蛋白Rad51抑制剂及抗肿瘤的活性。Phase 2。

Inactivation of AXL by MP470 reverses epithelial to mesenchymal transition. Immunoblot analyses of lysates from TGFβ/TNFα- treated MCF10A cells treated with varying amounts of MP470 for 72 hours.

S1164

Lenvatinib (E7080)是一种多靶点抑制剂，无细胞试验中，作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效，IC50为4 nM/5.2 nM，对VEGFR1/Flt-1作用效果稍弱，作用于VEGFR2/3比作用于FGFR1， PDGFRα/β选择性高10倍左右。Lenvatinib (E7080) 也是FGFR1-4、PDGFR、Kit (c-Kit)和RET (c-RET)的抑制剂，并具有强效的抗肿瘤活性。Phase 3。

Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.

S4947New

Regorafenib (Stivarga, BAY 73-4506) Hydrochloride 是一种多靶点抑制剂，对 VEGFR1、Murine VEGFR2/3、PDGFRβ、Kit (c-Kit)、RET (c-RET) 和 Raf-1 的IC50值分别为13 nM、4.2 nM/46 nM、22 nM、7 nM、1.5 nM和2.5 nM。

S2692

TG101209是一种选择性的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET (c-RET)作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。

EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (*,P < 0.05; **, P < 0.01; ***, P < 0.001; NS, nonsignificant).

S4001

Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐，是有效的VEGFR2抑制剂，IC50为0.035 nM，也抑制c-Met， RET (c-RET)， Kit (c-Kit)， Flt-1/3/4， Tie2和AXL，无细胞试验中IC50分别为1.3 nM， 4 nM， 4.6 nM， 12 nM/11.3 nM/6 nM， 14.3 nM和7 nM。Cabozantinib malate (XL184)可诱导细胞凋亡。

Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.

S8015

Agerafenib (RXDX-105, CEP-32496) 是一种高度有效的BRAF(V600E/WT)和c-Raf抑制剂，Kd为14 nM/36 nM和39 nM，适度有效作用于Abl-1， c-Kit， RET (c-RET)， PDGFRβ和VEGFR2，对MEK-1， MEK-2， ERK-1和ERK-2具有微弱的亲和力。Phase 1/2。

S8189

BAW2881 (NVP-BAW2881)是一种新型的VEGFR酪氨酸激酶抑制剂。在1.0-4.3 nM浓度下能有效地抑制VEGFR1-3；在45-72 nM的浓度下，抑制PDGFRβ, c-Kit和RET (c-RET)。

S6520

WHI-P180是多种激酶的抑制剂，对RET (c-RET)和KDR的IC50值分别为4.5 nM和66 nM。

S5240

Lenvatinib Mesylate (E7080)是一种合成、具有口服活性的 tyrosine kinase 的抑制剂，可抑制血管内皮生长因子受体(VEGFR1-3)，成纤维细胞生长因子受体(FGFR1-4)，血小板衍生生长因子受体(PDGFRα)，干细胞因子受体(Kit (c-Kit))，并在转染过程中重新排列(RET (c-RET))。甲磺酸来伐替尼具有潜在的抗肿瘤活性。

S8401

Erdafitinib (JNJ-42756493)是有效的、具有选择性和口服生物活性的泛成纤维细胞生长因子受体FGFR抑制剂，具有潜在的抗肿瘤活性。Erdafitinib 也能结合RET (c-RET)、CSF-1R、PDGFR-α/PDGFR-β、FLT4、Kit (c-Kit)和VEGFR-2并可诱导细胞凋亡。

E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493

S6662

AST-487 (NVP-AST487)，一种N,N'-二苯基脲，是Flt3的竞争性抑制剂，ki值为0.12 μM。除FLT3以外，AST487还抑制RET,KDR,c-KIT 和 c-ABL 激酶，IC50值低于1 μM。

S0377

CS-2660 (JNJ-38158471) 是一种耐受性良好的、口服有效的、高选择性的 VEGFR-2 抑制剂，IC50值为40 nM。CS-2660(JNJ-38158471)还抑制紧密相关的酪氨酸激酶，如 Ret (c-RET) 和 Kit (c-Kit)，IC50为180 nM和500 nM，但无明显活性 (>1 microM) 针对VEGFR-1和VEGFR-3。

S8161

ON123300是有效的多靶点激酶抑制剂，对CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。

S8716

Pralsetinib (BLU-667, CS 3009, Gavreto) 是一种高效的、选择性RET (c-RET)抑制剂，对WT RET (c-RET)的IC50值为0.4 nM。它对一些常见的RET (c-RET)致癌突变同样具有有效的抑制作用，IC50~0.4 nM。

S8696

2-D08 (2',3',4'-trihydroxy flavone) 是一种具有细胞透性的蛋白类泛素化(protein sumoylation)抑制剂。它还能抑制Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。

S8821

GSK3179106是有效的、选择性的RET (c-RET) kinase抑制剂，IC50为0.3 nM。

S8781

Selpercatinib (LOXO-292, ARRY-192)是一种有效、特异的RET (c-RET)抑制剂，对WT RET (c-RET), RET (c-RET) (V804M), RET (c-RET) (V804L), RET (c-RET) (A883F), RET (c-RET) (M918T)和RET (c-RET) (S891A)的IC50值分别为1 nM、2 nM、2 nmM、4 nM、2 nM和2 nM。

S5077

Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate 是一种新型口服的多重激酶抑制剂，对VEGFR1、小鼠VEGFR2、小鼠VEGFR3、PDGFR-β、Kit (c-Kit)、RET (c-RET)、RAF-1、B-RAF和B-RAF(V600E)的IC50分别为13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM。