靶向肿瘤武器:激酶抑制剂与临床相关产品

时间: 2026-01-19
作者: 百灵威
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肿瘤发生与发展过程中,异常活化的信号通路如PI3K/Akt/mTOR、MAPK、JAK-STAT等,扮演着驱动细胞增殖、存活、侵袭及血管生成的关键角色。针对这些通路中特异性激酶节点开发的抑制剂,已成为现代靶向治疗的支柱。其中,针对表皮生长因子受体的抑制剂能够阻断驱动非小细胞肺癌等肿瘤的生长信号;针对BRAF和MEK的抑制剂通过垂直抑制MAPK通路,有效对抗特定基因突变的黑色素瘤;BCR-ABL抑制剂则革新了慢性髓系白血病的治疗格局,将其转变为一种可管理的慢性病。此外,作用于血管内皮生长因子受体的抑制剂通过抑制肿瘤血管生成,切断其营养供给;而针对PI3K和JAK的抑制剂,则在血液肿瘤及免疫炎症相关疾病中展现出显著疗效。这些高度特异性的分子工具不仅为临床提供了多样化的治疗选择,也为深入探索肿瘤生物学、验证新靶点及克服耐药机制提供了不可或缺的研究手段,持续推动着个体化精准医疗的边界。

百灵威提供各类小分子抑制剂,助力信号通路研究及新药筛选。 靶点清晰明确,便于选择; 严格的质检,确保产品高纯度、高品质; 生物活性经多客户验证。
EGFR抑制剂
品名 CAS 货号
Gefitinib, 99%
吉非替尼
184475-35-2 125560
Erlotinib hydrochloride, 98.5%
埃罗替尼盐酸盐
183319-69-9 341250
Osimertinib, 98%, a potent and selective mutated forms EGFR inhibitor
迈瑞替尼
1421373-65-0 1761088
Afatinib, 99%, inhibits EGFR/ErbB irreversibly
阿法替尼
439081-18-2 1232626
BRAF抑制剂
品名 CAS 货号
Vemurafenib, 99%, a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively
维罗非尼
918504-65-1 1349108
Dabrafenib, 98%, a mutant BRAFV600 specific inhibitor
达拉菲尼
1195765-45-7 1410144
MEK抑制剂
品名 CAS 货号
Trametinib, 98%, a MEK1/2 inhibitor
曲美替尼
871700-17-3 1239133
Cobimetinib, 98%
卡比替尼
934660-93-2 1434274
SL327, 98%, inhibits MEK1 and MEK2
SL327抑制剂
305350-87-2 188536
U0126-EtOH, 98%, a high selective MEK1/2 inhibitor
U0126-EtOH抑制剂
1173097-76-1 1759173
PD0325901, 98%, a selective and cell permeable MEK inhibitor with an IC50 of 0.33 nM
PD0325901抑制剂
391210-10-9 837005
PD98059, 98%, a non-ATP competitive MEK inhibitor
PD98059抑制剂
167869-21-8 302058
JAK抑制剂
品名 CAS 货号
Tofacitinib citrate, 99%, an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively
柠檬酸托法替尼
540737-29-9 1430418
Ruxolitinib, 98%, a potent and selective JAK1/2 inhibitor
鲁索利替尼
941678-49-5 975111
VEGFR抑制剂
品名 CAS 货号
Sunitinib, 98%, a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively
苏尼替尼
557795-19-4 381939
Sorafenib, 98%
索拉非尼
284461-73-0 297281
Pazopanib, 98%, a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively
帕唑帕尼
444731-52-6 981527
BCR-ABL抑制剂
品名 CAS 货号
Imatinib, 98%, an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity
伊马替尼
152459-95-5 993508
Dasatinib, 98%, a dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC50s of 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit and c-KitD816V, respectively
达沙替尼
302962-49-8 923898
Nilotinib, 98%, an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity
尼罗替尼
641571-10-0 906995
选择性PI3激酶抑制剂
品名 CAS 货号
LY-294,002 hydrochloride, 98%, selective inhibitor of PI 3-kinase
LY-294,002盐酸盐
934389-88-5 1093593
2-Morpholino-8-phenylchromone, 98%, a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively
2-吗啉代-8-苯基色酮
154447-36-6 284107
Alpelisib, 98%, a potent and selective PI3Kα inhibitor
阿培利司
1217486-61-7 1004472
Rociletinib, 98%, an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
罗乐替尼
1374640-70-6 1684920
仪器耗材
品名 CAS 货号
T25 c㎡ NPsurface cell culture bottle, Bag sterilization, white breathable cover, 12 pieces/bag, 25 bags/box
T25c㎡ NPsurface细胞培养瓶
/ 9451491
100mm TC cell culture dish, Sterilized bagged, 10 tips/pack, 30 packs/case
100mm TC细胞培养皿
/ 9451994
1.5mL Protein low-adhesion centrifuge tube, Sterilized bagged, transparent, 10 tips/pack, 10 packs/box, 10 boxes/case
1.5mL蛋白低吸附离心管
/ 9451926
2mL Protein low-adhesion centrifuge tube, Sterilized bagged, transparent, 10 tips/pack, 10 packs/box, 10 boxes/case
2mL蛋白低吸附离心管
/ 9451943
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