高活性小分子抑制剂、激动剂——靶点清晰明确，便于选择-百灵威

研究表明，肿瘤、代谢性疾病等的发生、发展与细胞信号通路异常密切相关^[1-3]。小分子抑制剂可作用于通路靶标蛋白，阻断信号传递，广泛用于信号通路基础研究及药物发现中。

其中，以蛋白酪氨酸激酶（PTK）为靶点的药物研发已成为当前肿瘤药物研究的热点之一，PTK功能失调会导致下游信号通路激活，进而引起细胞增殖调节紊乱。目前国内外已有十几种以酪氨酸激酶（TK）为靶点的激酶抑制剂类抗肿瘤药物上市，而且还有大量的化合物处于临床前研究或临床试验阶段，这些药物的出现为肿瘤治疗提供了新方向^[4]。

百灵威提供20多种通路中的抑制剂、激动剂等活性小分子化合物，可作用于PI3K/Akt/mTOR、PTK、Apoptosis、Cell Cycle/DNA Damage、JAK/STAT等热门信号通路靶点（图1）。

靶点清晰明确，便于选择；
严格质检，确保产品高纯度、高品质；
活性高，生物活性经多客户验证；
90%以上有现货，可大量供应，满足动物实验需求；
产品数量持续增长；
性价比高：同比每个产品可节约5%-20%成本。

图1 百灵威提供20多种通路中的小分子抑制剂、激动剂

GPCR & G 蛋白信号通路

品名	产品描述	货号&CAS
Atomoxetine hydrochloride, 99% 盐酸托莫西汀	a selective norepinephrine reuptake inhibitor	506507 82248-59-7
Escitalopram oxalate, 98% 草酸右旋西酞普兰	a selective serotonin reuptake inhibitor	317177 219861-08-2
Granisetron hydrochloride, 98% 盐酸格拉司琼	a serotonin 5-HT3 receptor antagonist	384285 107007-99-8
Levosulpiride, 98% 左旋舒必利	a selective antagonist for D2 dopamine receptor	519766 23672-07-3
Naftopidil, 98% 萘哌地尔	a selective α1-adrenergic receptor antagonist	434183 57149-07-2
Olopatadine hydrochloride, 99% 盐酸奥洛他定	a selective H1 receptor antagonist	156717 140462-76-6
Plerixafor, 99% 普乐沙福	a selective CXCR4 antagonist with an IC50 of 44 nM	993174 110078-46-1
Xylometazoline hydrochloride, 98% 盐酸赛洛唑啉	an α-adrenoceptor agonist	304079 1218-35-5

DNA损伤信号通路

品名	产品描述	货号&CAS
Bendamustine hydrochloride, 98% 盐酸苯达莫司汀	a DNA-damaging agent	591713 3543-75-7
Chebulinic acid, 98% 诃子林鞣酸	a potent natural inhibitor of M. tuberculosis DNA gyrase	150210 18942-26-2
Ciprofibrate, 99% 环丙贝特	a PPAR α agonist	398914 52214-84-3
Fludarabine, 99% 氟达拉宾碱	a DNA synthesis and methylation inhibitor	955789 21679-14-1
Flupirtine maleate salt, 97% 马来酸氟吡汀	a selective neuronal potassium channel opener, NMDA receptor antagonist	904475 75507-68-5
Teniposide, 98% 替尼泊苷	N/A	563738 29767-20-2
Tubastatin A HCl, 98% 新橙皮苷二氢查耳酮	a potent and selective HDAC6 inhibitor	1564431 1310693-92-5

蛋白质酪氨酸激酶信号通路

品名	产品描述	货号&CAS
R-Afatinib, 98% R-阿法替尼	an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively	996037 850140-72-6
Axitinib, 98% 阿西替尼	a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively	812864 319460-85-0
Crizotinib, 98% 克唑替尼	an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM	1019251 877399-52-5
Dasatinib monohydrate, 99% 达沙替尼单水合物	a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM	1020809 863127-77-9
Lapatinib, 98% 拉帕替尼	a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively	831262 231277-92-2
Lapatinib ditosylate, 98% 二甲苯磺酸拉帕替尼	a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively	795123 388082-77-7
Sunitinib malate, 98% 苹果酸舒尼替尼	a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively	1020808 341031-54-7

细胞周期信号通路

品名	产品描述	货号&CAS
Chebulinic acid, 98% 诃子林鞣酸	a potent natural inhibitor of M. tuberculosis DNA gyrase	150210 18942-26-2
Fasudil hydrochloride, 98% 盐酸法舒地尔	a nonspecific ROCK inhibitor , with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively	101990 105628-07-7
Irinotecan, 99% 伊立替康	a water soluble topoisomerase I inhibitor	130846 97682-44-5
SNS-032, 99% SNS-032	a selective CDK2 inhibitor	1004546 345627-80-7