产品编号 | 产品名称 | 产品简述 | 应用领域 | 参考文献 | 客户反馈 |
Erlotinib HCl (OSI-744) | Erlotinib HCl (OSI-744)是用于治疗非小细胞肺癌(NSCLC),胰腺癌和其它几种类型癌症的药物。 |
肺癌,胰腺癌 |
Avan A, et al. Cancer Res, 2013, 73(22), 6745-6756. Surriga O, et al. Mol Cancer Ther, 2013, 12(12), 2817-2826. Sun Y, et al. Mol Cancer Ther, 2013, 12(5), 696-704. Eswaraka J, et al. BMC Cancer, 2014, 14, 742. |
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Crizotinib (PF-02341066) | Crizotinib (PF-02341066)是一种抗癌药物,ALK和ROS1抑制剂,用于治疗非小细胞肺癌(NSCLC)。 |
肺癌 |
Avan A, et al. Cancer Res, 2013, 73(22), 6745-6756. Surriga O, et al. Mol Cancer Ther, 2013, 12(12), 2817-2826. Sun Y, et al. Mol Cancer Ther, 2013, 12(5), 696-704. Eswaraka J, et al. BMC Cancer, 2014, 14, 742. |
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Gefitinib (ZD1839) | Gefitinib 是用于治疗乳房,肺和其它的肿瘤。 |
肺癌 |
Kim SC, et al. J Control Release, 2001, 72(1-3), 191-202. Dominguez-Escrig JL, et al. Clin Cancer Res, 2004, 10(14), 4874-4884. Ishii Y, et al. Am J Respir Crit Care Med, 2006, 174(5), 550-556. Kang BK, et al. Int J Pharm, 2004, 286(1-2), 147-156. |
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Cabozantinib (XL184, BMS-907351) | Cabozantinib (XL184, BMS-907351)是一种口服生物可利用酪氨酸激酶抑制剂,阻断MET,VEGRF2和RET,并对甲状腺髓样癌有相当的活性。 |
甲状腺癌,肾细胞癌 |
Yakes FM, et al. Mol Cancer Ther, 2011, 10(12), 2298-2308. Dai J, et al. Clin Cancer Res, 2014, 20(3), 617-630. Zhu Z, et al. J Control Release. 2010, 142(3), 438-446. Nguyen HM, et al. PLoS One, 2013, 8(10), e78881. |
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Regorafenib (BAY 73-4506) | Regorafenib (BAY 73-4506)显示抗血管生成活性,由于双重的酪氨酸激酶抑制作用。 |
结肠直肠癌,胃肠道间质瘤 |
Wilhelm SM, et al. Int J Cancer, 2011, 129(1), 245-255. Danhier F, et al. J Control Release, 2009, 133(1), 11-17. Schmieder R, et al. Int J Cancer, 2014, 135(6), 1487-1496. Cyran CC, et al. PLoS One, 2013, 8(9), e76009. |
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Ponatinib (AP24534) | Ponatinib (AP24534)是一种口服药物,用于治疗慢性髓细胞样白血病和费城染色体阳性(PH)急性淋巴细胞白血病。 |
白血病 |
Ishitsuka K, et al. Br J Haematol, 2008, 141(5), 598-606. Tate CM, et al. J Biol Chem, 2013, 288(9), 6743-6753. Campbell RM, et al. Mol Cancer Ther, 2014, 13(2), 364-374. Naka K, et al. Nat Commun, 2015, 6, 8039. |
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Afatinib (BIBW2992) | Afatinib (BIBW2992)是受体酪氨酸激酶表皮生长因子受体(EGFR)和erbB-2的(HER2)的不可逆共价抑制剂。 |
肺癌 |
Ninomiya T, et al. Mol Cancer Ther, 2013, 12(5), 589-597. Tsai YC, et al. Eur J Cancer, 2013, 49(6), 1458-1466. Wang XK, et al. Oncotarget, 2014, 5(23), 11971-11985. Guan SS, et al. Oncotarget, 2014, 5(13), 4868-4880. |
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Cabozantinib S-Malate | Cabozantinib S-Malate是一种口服生物可利用酪氨酸激酶抑制剂,阻断MET,VEGRF2和RET,并对甲状腺髓样癌有相当的活性。 |
甲状腺癌 |
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Sunitinib Malate | Sunitinib Malate是多靶点RTK抑制剂,作用于VEGFR2 (Flk-1)和PDGFR-beta。 |
肾癌,胃肠道间质瘤 |
Mendel DB, et al. Clin Cancer Res, 2003, 9(1), 327-337. O'Farrell AM, et al. Blood, 2003, 101(9), 3597-3605. Ebos JM, et al. Cancer Cell, 2009, 15(3):232-239. Tang SC, et al. Int J Cancer, 2012, 130(1):223-233. |
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Imatinib Mesylate (STI571) | Imatinib Mesylate (STI571)是口服的v-Abl, c-Kit 和PDGFR多靶点抑制剂。 |
胃肠肿瘤,白血病 |
Decaudin D, et al. Int J Cancer. 2005, 113(5), 849-856. Gambacorti-Passerini C,et al. J Natl Cancer Inst, 2000, 92(20):1641-1650. Hwang RF, et al. Clin Cancer Res, 2003, 9(17):6534-6544. Zheng Hu, et al. PLoS One, 2009, 4(7): e6257. |
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Lapatinib (GW-572016) Ditosylate | Lapatinib (GW-572016) Ditosylate是一种EGFR/ErbB2抑制剂,主要用于抑制ErbB过表达乳腺癌细胞系的生长。 |
乳腺癌 |
Rusnak DW, et al. Mol Cancer Ther, 2001, 1(2), 85-94. Gril B,et al. J Natl Cancer Inst, 2008, 100(15):1092-1103. Taskar KS, et al. Pharm Res, 2012, 29(3):770-781. Strecker TE, et al. J Natl Cancer Inst, 2009, 101(2):107-113. |
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Nilotinib (AMN-107) | Nilotinib (AMN-107)是Bcr-Ab抑制剂,用于治疗Imatinib耐药的慢性髓性白血病。 |
白血病 |
Weisberg E, et al. Cancer Cell. 2005, 7(2), 129-141. Shaker ME,et al. Toxicol Appl Pharmacol, 2011, 252(2):165-175. Kaur P, et al. Mol Cancer, 2007, 6:67. Wei J, et al. PLoS One, 2014, 9(10):e107760. |
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Nintedanib (BIBF 1120) | Nintedanib (BIBF 1120)是多种酪氨酸(PDGFR,VEGFR,FGFR)抑制剂,用于治疗非小细胞肺癌与特发性纤维化。 |
肺癌 |
Hilberg F, et al. Cancer Res, 2008, 68(12), 4774-4782. Roth GJ, et al. J Med Chem, 2009, 52(14), 4466-4480. Kutluk Cenik B, et al. Mol Cancer Ther, 2013, 992-1001. Kudo K, et al. Clin Cancer Res, 2011,17(6):1373-1381. |
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Linsitinib (OSI-906) | Linsitinib (OSI-906)是有效的,口服型IGF-1R(胰岛素样生长因子受体1)和IR(胰岛素受体)双重抑制剂。 |
前列腺癌,胃肠肿瘤,尤因氏肉瘤 |
Mulvihill MJ, et al. Future Med Chem, 2009, 1(6), 1153-1171. McKinley ET, et al. Clin Cancer Res, 2011, 17(10), 3332-3340. Flanigan SA, et al. Clin Cancer Res, 2013, 19(22):6219-6229. Leiphrakpam PD, et al. Oncol Rep, 2014, 31(1):87-94. |
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Pazopanib (GW786034) HCl | Pazopanib (GW786034) HCl多靶点激酶抑制剂,用于治疗晚期肾细胞癌、软组织肉瘤、晚期卵巢癌。 |
肾细胞癌,软组织肉瘤 |
Hosaka S, et al. J Orthop Res. 2012. Kumar R, et al. Mol Cancer Ther, 2007, 6(7):2012-2021. Harris PA, et al. J Med Chem, 2008, 51(15):4632-4640. Podar K, et al. Proc Natl Acad Sci U S A, 2006, 103(51):19478-19483. |
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Foretinib (GSK1363089) | Foretinib (GSK1363089)是Met/RON/Axl/VEGFR多靶点抑制剂,能直接影响细胞增殖、抑制肿瘤细胞入侵和血管生成。 |
肺癌,乳腺癌 |
Qian F, et al. Cancer Res, 2009, 69(20), 8009-8016. You WK, et al. Cancer Res, 2011, 71(14):4758-4768. Zillhardt M, et al. Clin Cancer Res, 2011, 17(12):4042-4051. Davare MA, et al. Proc Natl Acad Sci U S A, 2013, 110(48):19519-19524. |
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R428 (BGB324) | R428(BGB324)是Axl受体酪氨酸激酶的有效和选择性抑制剂,在非小细胞肺癌的临床试验中。 |
肺癌,白血病 |
[1] Holland SJ, et al. Cancer Res, 2010, 70(4), 1544-1554. [2] Tong LS, et al. J Cereb Blood Flow Metab, 2016, pii: 0271678X16658490. [3] Wang C, et al. Theranostics, 2016, 6(8), 1205-1219. [1] Holland SJ, et al. Cancer Res, 2010, 70(4), 1544-1554. |
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Crenolanib (CP-868596) | Crenolanib (CP-868596)是一种有效的、选择性的PDGFR alpha/beta的ATP竞争性抑制剂,临床上具有治疗Flt3-ITD或AL突变的AML患者的潜能。 |
胃肠肿瘤,白血病 |
Zimmerman EI, et al. Blood, 2013, 122(22):3607-3615. Wang P,et al. Onco Targets Ther, 2014,7:1761-1768. |
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Neratinib (HKI-272) | Neratinib (HKI-272)是非可逆的口服ErbB抑制剂,通过抑制ErbB1/2/4来阻断信号传导,用于治疗实质固态瘤比如乳腺癌。 |
乳腺癌 |
Rabindran SK, et al. Cancer Res, 2004, 64(11), 3958-3965. Li D,et al. Cancer Cell, 2007, 12(1):81-93. Ji H, et al. Cancer Cell, 2006, 9(6):485-495. |
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TAE684 (NVP-TAE684) | TAE684(NVP-TAE684)在治疗非小细胞肺癌的临床试验中是一种有效的选择性ALK抑制剂。 |
[1] Galkin AV, et al. Proc Natl Acad Sci U S A, 2007, 104(1), 270-275. [2] Yang L, et al. Tumour Biol, 2014, 35(10), 9759-9767. [3] Heukamp LC, et al. Sci Transl Med, 2012, 4(141),141ra91. [4] Katayama R, et al. Proc Natl Acad Sci U S A, 2011, 108(18), 7535-7540. |
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PHA-665752 | PHA-665752是ATP竞争性的,抑制c-Met活化位点的激酶抑制剂,对c-Met的选择性比其他酪氨酸和丝氨酸-苏氨酸激酶高50倍。 |
胃癌 |
Christensen JG, et al. Cancer Res, 2003, 63(21), 7345-7355. Puri N,et al. Cancer Res, 2007, 67(8):3529-3534. Yang Y, et al. Mol Cancer Ther, 2008, 7(4):952-960. |
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Axitinib | Axitinib是多靶点抑制剂,抑制VEGFR1/2/3,PDGFR-beta和c-Kit,用于治疗进展性肾细胞癌。 |
肾细胞癌 |
Hu-Lowe DD, et al. Clin Cancer Res, 2008, 14(22), 7272-7283. Rossler, J. et al., Int J Cancer, 2011, 128(11), 2748-2758. Wilmes LJ, et al. Magn Reson Imaging, 2007, 25(3):319-327. Hillman GG, et al. Transl Oncol, 2014, pii: S1936-5233(14)00037-0. |
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Vandetanib (ZD6474) | Vandetanib (ZD6474)是VEGF flk-1/KDR receptor (VEGFR-2)抑制剂,是首个治疗甲状腺髓样癌的药物。 |
甲状腺癌 |
Wedge SR, et al. Cancer Res. 2002, 62(16), 4645-4655. Ciardiello F, et al. Clin Cancer Res. 2003, 9(4), 1546-1556. Hennequin LF, et al. J Med Chem, 2002, 45(6):1300-1312. Williams KJ, et al. Clin Cancer Res, 2004, 10(24):8587-8593. |