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Raf inhibitor
索拉非尼酯（Nexavar）是一种新型小分子抑制剂，能够抑制多种酪氨酸蛋白激酶（VEGFR 和 PDGFR）以及 RAF/MEK/ERK 信号通路，对 Raf-1、野生型 BRAF 和 V599E 突变型 BRAF 的半抑制浓度（IC50）分别为 6、22、38 nM。- Arda Kipcak, .et al. , Mol Biol Rep, 2024, Jul 13;51(1):799 PMID: 39001931
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. , Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. , J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. , Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. , J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. , Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. , J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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VEGFR/PDGFR inhibitor
Linifanib（ABT-869）是一种结构新颖的强效抑制剂，针对RTK、VEGF和PDGF具有显著抑制作用，其IC50分别为针对人类内皮细胞、PDGFR-β、KDR和CSF-1R的0.2、2、4和7 nM。
- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
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FLT3 inhibitor
AC220（Quizartinib）是一种独特的高效和选择性的FLT3抑制剂，其IC50为0.56±0.3 nM，对MC4-11和A375的IC50则大于10 mM。- Nicholas R Anderson, .et al. , Leukemia, 2023, Mar;37(3):560-570 PMID: 36550214
- N Naganna, .et al. , EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Cong Li, .et al. , Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Yaping Zhang, .et al. , J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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EGFR inhibitor
AEE788 是一种口服生物可利用的多受体酪氨酸激酶抑制剂，能够抑制 EGFR、HER2 和 VEGF2 的酪氨酸激酶的磷酸化。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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EGFR inhibitor
AG 490 是一种选择性的 EGF 受体酪氨酸激酶抑制剂（EGFR 和 ErbB2 的 IC50 值分别为 2 和 13.5 μM）。同时抑制 JAK2，对 Lck、Lyn、Btk、Syk 和 Src 无活性。- Matozaki M, .et al. , Exp Cell Res, 2019, Feb 15. pii: S0014-4827(18)31030-9 PMID: 30776355
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EGFR inhibitor
AST-6 是一种新型不可逆的表皮生长因子受体1和2的抑制剂，能够在体外和体内抑制肿瘤生长。 -
BCR-ABL inhibitor
AP24534（Ponatinib）是一种强效的多激酶和全谱BCR-ABL抑制剂。- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. , Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. , EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. , Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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VEGFR Inhibitor
Tivozanib（AV-951）是一种口服 VEGF 受体酪氨酸激酶抑制剂，旨在抑制所有三种 VEGF 受体。- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 45954 PMID: 28383032
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 44075 PMID: 28287096
- Nicholas A. Manieri, .et al. , J Clin Invest, 2015, Sep 1; 125(9): 3606-3618 PMID: 26280574
- Usui T, .et al. , Acta Physiol (Oxf), 2014, 211, 385-394 PMID: 24612679
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VEGFR inhibitor
Axitinib 是一种小分子酪氨酸激酶抑制剂，它能抑制多个靶点，包括 VEGFR-1、VEGFR-2、VEGFR-3、血小板源生长因子受体（PDGFR）和 cKIT (CD117)。- Sophie J. Bakri, .et al. , PLoS One, 2024, 19(6): e0304782 PMID: 38833447
- Hongwan Ding, .et al. , Toxicol Appl Pharmacol, 2024, May:486:116950 PMID: 38701902
- Hongwan Ding, .et al. , Research Square, 2023, Dec 28
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Youcef M. Rustum, .et al. , Int J Mol Sci, 2018, Nov; 19(11): 3378 PMID: 30380599
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Src/Abl inhibitor
Saracatinib (AZD0530) 是一种高度选择性的、可口服的双特异性 Src/Abl 激酶抑制剂，其对 c-Src 和 Abl 激酶的 IC50 分别为 2.7 nM 和 30 nM。- Andromachi Lambrianidou, .et al. , Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Chisato Naito, .et al. , Atherosclerosis, 2016, Mar;246:344-51 PMID: 26828753
- Kenta Maruyama, .et al. , J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 PMID: 25691576
- Amanda L Jackson, .et al. , Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 PMID: 26001052
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pan-EGFR/pan-erbB inhibitor
AZD8931 是一种口服的、对 ErbB1、ErbB2 和 ErbB3 受体信号传导具有同等抑制作用的抑制剂。- Takeshi Ito, .et al. , Biochem Biophys Res Commun, 2019, in Press
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VEGFR inhibitor
BIBF1120（Vargatef）是一种新型的三重血管激酶抑制剂，能同时抑制三种生长因子受体：VEGFR、PDGF 和 FGFR。- Yan Yang, .et al. , J Thorac Dis, 2024, Feb 29;16(2):1128-1140 PMID: 38505034
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Chun-Jung Chang, .et al. , Biochem Pharmacol, 2021, Jan;183:114356 PMID: 33285108
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EGFR inhibitor
BIBW2992（阿法替尼）是一种酪氨酸激酶抑制剂（TKI），可以不可逆地抑制人类表皮生长因子受体2（Her2）和表皮生长因子受体（EGFR）激酶。- Song Han, .et al. , Neoplasia, 2025, Jan:59:101070 PMID: 39541736
- Sang-Hyun Lee, .et al. , NPJ Precis Oncol, 2024, May 21;8(1):111 PMID: 38773241
- Yi-Ru Pan, .et al. , Int J Biol Sci, 2023, May 21;19(9):2772-2786 PMID: 37324940
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Van Sebille YZ, .et al. , Exp Biol Med (Maywood), 2019, Jun 11:1535370219855334 PMID: 31184924
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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c-Met inhibitor
BMS-777607 是一种 MET 酪氨酸激酶抑制剂，它与 c-Met 蛋白（或 HGFR）结合，阻止 HGF 的结合并中断 MET 信号通路。 -
c-Met inhibitor
BMS-794833 是一种强效的 ATP 竞争性抑制剂，针对 Met 和 VEGFR-2，其 IC50 分别为 1.7 和 15 纳摩尔。 -
Src inhibitor
Bosutinib (SKI-606) 是一种酪氨酸激酶抑制剂，正在研究中用于治疗癌症。- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
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VEGFR inhibitor
Brivanib alaninate (BMS-582664) 是一种针对 VEGFR 和 FGFR 信号传导的双重酪氨酸激酶抑制剂。 -
VEGFR inhibitor
Cediranib (AZD2171) 是一种强效的血管内皮生长因子 (VEGF) 受体酪氨酸激酶抑制剂。- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
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RTK inhibitor
Dovitinib 是一种小分子多靶点受体酪氨酸激酶抑制剂，它能够抑制通过 ZNF198-FGFR1 或 BCR-FGFR1 转化为 IL3 独立的 Ba/F3 细胞，其 IC50 值分别为 150 nM 和 90 nM。 -
EGFR inhibitor
Chrysophanic acid (Chrysophanol) 通过抑制 EGFR/mTOR 通路来阻止结肠癌细胞的增殖。 -
HER2/ErbB2 inhibitor
Canertinib (CI-1033) 是一种不可逆的酪氨酸激酶抑制剂，对 EGFR (IC50 0.8 nM)、HER-2 (IC50 19 nM) 和 ErbB-4 (IC50 7 nM) 有活性。- Fukuda N, .et al. , ACS Synth Biol., 2015, 4(4):421-9 PMID: 25006755
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HER2/ErbB2 inhibitor
CP-724714 是一种口服的小分子药物，是一种强效的 HER-2酪氨酸激酶抑制剂，能够抑制 HER2 激酶（IC50 为 3.8 ng/ml）。- Yu Muta, .et al. , Nat Commun, 2018, 9: 2174 PMID: 29872037
- Gina M. Sizemore, .et al. , Nat Commun, 2018, 9: 2783 PMID: 30018330
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VEGFR inhibitor
Regorafenib（BAY 73-4506）是一种多激酶抑制剂，其IC50分别为17、40和69 nM的c-KIT、VEGFR2、B-Raf。Regorafenib（BAY 73-4506）是一种口服生物可用的多激酶抑制剂，针对肿瘤及其血管系统。- Hasan U, .et al. , Research Square, 2023, 13 Apr
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. , Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. , Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. , Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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VEGFR-2 inhibitor
Brivanib（BMS-540215）是一种VEGFR-2抑制剂，其IC50为25 nM，Ki为26 nM。- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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PDGFR inhibitor
Imatinib (Gleevec) 是一种针对酪氨酸激酶酶的特异性抑制剂。- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Takafumi Shima, .et al. , Oncol Rep, 2022, 47: 7 PMID: 34738628
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- BM Duggan, .et al. , Endocrinology, 2020, May 30;bqaa086 PMID: 32473019
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
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Abl-Src inhibitor
Dasatinib（BMS-354825）是一种口服多效 BCR/ABL 和 Src 家族酪氨酸激酶抑制剂。Dasatinib 的主要靶点包括 BCR/ABL、Src、c-Kit、ephrin 受体以及其他几种酪氨酸激酶，但不包括 erbB 激酶，如 EGFR 或 Her2。- Hiroyasu Aoki, .et al. , Cell Rep, 2024, Mar 26;43(3):113887 PMID: 38458195
- Hiroto Kataoka, .et al. , Anal Biochem, 2023, Oct 1;678 PMID: 37541642
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Chihiro Motozono, .et al. , Nat Commun, 2022, Sep 21;13(1):5440 PMID: 36130929
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Adi Jacob Berger, .et al. , Nat Cancer, 2021, 2, 1055-1070 PMID: 35121883
- David E J Klawon, .et al. , J Exp Med, 2021, Jun 7;218(6) PMID: 33914024
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Sano T, .et al. , Am J Pathol, 2018, Nov;188(11):2564-2573 PMID: 30121259
- Ines Peschel, .et al. , Haematologica, 2017, Aug; 102(8): 1378-1389 PMID: 28522571
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- John D. Leonard, .et al. , Immunity, 2017, Jul 18; 47(1): 107-117.e8 PMID: 28709804
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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VEGFR Inhibitor
E7080 是一种多激酶抑制剂，能够抑制 VEGFR2 和 VEGFR3 激酶。- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Mai Nakahara, .et al. , Biomed Rep, 2022, Aug 3;17(4):78 PMID: 36158319
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Keisuke Enomoto, .et al. , Cancers (Basel), 2021, Feb 18;13(4):862 PMID: 33670725
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Koide H, .et al. , Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Tomoko Ogawa-Morita, .et al. , Int J Anal Chem, 2017, 2017: 2341876 PMID: 28680445
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EGFR inhibitor
Erlotinib hydrochloride 是一种可逆的酪氨酸激酶抑制剂，它作用于表皮生长因子受体（EGFR）。- Yuta Yamamoto, .et al. , J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Aikawa S, .et al. , Biochem Biophys Res Commun, 2017, Feb 26;484(1):202-208 PMID: 28073697
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EGFR Inhibitor
Gefitinib 是一种 EGFR 抑制剂，它通过干扰靶细胞中的表皮生长因子受体（EGFR）信号传导。- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Mansi Srivastava, .et al. , Int Immunopharmacol, 2019, 71: 188-197 PMID: 30909134
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Bcr-Abl inhibitor
伊马替尼甲磺酸盐是一种选择性酪氨酸激酶抑制剂，通过抑制KIT信号传导途径，在治疗胃肠间质瘤中诱导了持续的客观反应。- Inge Govaerts, .et al. , J Hematol Oncol, 2021, 14: 97 PMID: 34167562
- Genevra Kuziel, .et al. , Cancers (Basel), 2020, Jul 28;12(8):E2083 PMID: 32731354
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c-Met inhibitor
c-Met 抑制剂 JNJ-38877605 选择性地结合到 c-Met，从而抑制 c-Met 磷酸化并干扰 c-Met 信号传导途径。 -
VEGFR-2 inhibitor
Ki8751 是一种细胞渗透性喹诺氧基苯基脲化合物，它在细胞内和细胞外实验中作为 Flk-1 (VEGFR-2) -选择性抑制剂。- Kohei Ashina, .et al. , Biochem Biophys Res Commun, 2015, Aug 21;464(2):590-5 PMID: 26163262
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c-Kit inhibitor
Masitinib (AB1010) 是一种蛋白酪氨酸激酶抑制剂。 -
c-Met inhibitor
MGCD265 是一种多靶点酪氨酸激酶抑制剂，它能结合并抑制多种受体酪氨酸激酶（RTKs）的磷酸化，包括 c-Met 受体（HGFR）；Tek/Tie-2 受体；VEGFR 类型 1、2 和 3；以及 MST1R。 -
VEGFR inhibitor
Motesanib，也被称为 AMG-706，是一种口服多激酶抑制剂，它选择性地针对 VEGF 受体、血小板源生长因子受体 和 Kit 受体。 -
HER2/ErbB2 inhibitor
Mubritinib (TAK 165) 是一种强效的 EGFR 和 p34cdc2 抑制剂，其 IC50 分别为 6 nM 和 0.2 μM。Mubritinib (TAK 165) 还能抑制 p33cdk2 和 p33cdk5。 -
HER2 inhibitor
Neratinib (HKI-272) 是一种酪氨酸激酶抑制剂。- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
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IGF-1R inhibitor
NVP-ADW742 是一种 IGF-1R 抑制剂，其 IC50 为 0.17 微摩尔。- Kazuya Takayama, .et al. , Sci Rep, 2018, 8: 8278 PMID: 29844341
- Kentaro Hirose, .et al. , BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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EphB4 inhibitor
NVP-BHG712 是一种选择性的 EphB4 激酶 抑制剂，在体外对 EphB4 的选择性优于40多种其他激酶，包括 FGFR3。- Ryuzaburo Yuki, .et al. , Eur J Pharmacol, 2024, Jan 15:963:176229 PMID: 38072041
- Y Kaibori, .et al. , the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
