Tyrosine Kinase(酪氨酸激酶)

Cat.No. 产品名称 Information

GC62268 SYN1143

N-[3-氟-4-[(7-甲氧基喹啉-4-基)氧基]苯基]-1-(2-羟基-2-甲基丙基)-5-甲基-3-氧代-2-苯基-2,3-二氢-1H-吡唑-4-甲酰胺

AMG-1 (c-Met/RON Dual Kinase Inhibitor, RON-IN-1) is a potent inhibitor of human c-Met and RON with IC50 of 4 nM and 9 nM, respectively.

GC62266 XL092

XL092

XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.

GC62260 TPX-0131

TPX-0131

TPX-0131 是一种有效、选择性、CNS 渗透性和口服活性的野生型 ALK 抑制剂 (IC50 为 1.4 nM) 和 ALK 抗性突变，例如 G1202R (IC50 为 0.3 nM)、L1196M (IC50 为 0.3 nM)。TPX-0131 具有很强的抗肿瘤活性。

GC62207 Olverembatinib

GZD824; HQP1351

A Bcr/Abl inhibitor

GC62197 PROTAC IRAK4 degrader-1 PROTAC IRAK4 degrader-1 是一种 PROTAC IRAK4 降解剂，详细信息请参考专利文献 US20190192668A1 中的化合物 I-210。PROTAC IRAK4 degrader-1 浓度为 0.01，0.1 和 1 μM 时作用于 OCI-LY-10 细胞，分别造成 20-50% 和 >50% IRAK4 蛋白降解。

GC62185 Axitinib-d3

AG-013736-d3

Axitinib-d3 是氘标记的 Axitinib。Axitinib 是多靶点的酪氨酸激酶抑制剂，抑制 VEGFR1，VEGFR2，VEGFR3， PDGFRβ 的 IC50 值分别为4，20，4，2 nM。

GC62160 Mobocertinib succinate

莫博替尼琥珀酸盐; TAK-788 succinate; AP32788 succinate

An inhibitor of mutant EGFR and HER2 receptors

GC62159 Tucatinib hemiethanolate

妥卡替尼半乙醇合物,Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate

An inhibitor of HER2

GC62146 XST-14 XST-14 是一种有效的，竞争性强且高度选择性的 ULK1 抑制剂，IC50 为 26.6 nM。XST-14 通过减少 ULK1 下游底物的磷酸化来诱导自噬抑制。XST-14 诱导肝细胞癌 (HCC) 细胞凋亡，并具有抗肿瘤作用。

GC62145 Chiauranib

CS2164

Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.

GC62114 Seralutinib

GB002; PK10571

Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively.

GC62112 Zotiraciclib Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.

GC62111 PND-1186 hydrochloride

VS-4718 hydrochloride; SR-2516 hydrochloride

A potent FAK inhibitor

GC62107 DGY-06-116 DGY-06-116 is an irreversible covalent and selective inhibitor of Src with IC50 of 2.6 nM.

GC62103 Vodobatinib

K0706

Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively.

GC61957 SU4984 SU4984 是一种蛋白质酪氨酸激酶抑制剂，抑制成纤维细胞生长因子受体 1 (FGFR1) 的 IC50 值为 10-20 µM。SU4984 还可抑制血小板衍生的生长因子受体和胰岛素受体的活性。SU4984 可用于癌症研究。

GC61944 IRAK4-IN-6 IRAK4-IN-6 是一种口服高效、选择性 IRAK 抑制剂，IC50 为 4 nM，靶向 MyD88 L265P 突变型弥漫性大 B 细胞淋巴瘤。

GC61942 Syk-IN-1 Syk-IN-1 (compound 4) 是一种有效的 Syk 抑制剂，IC50为 35 nM。

GC61852 PF-4618433 PF-4618433 是一种有效的、选择性的 PYK2 抑制剂，IC50 值为 637 nM。PF-4618433 可能适用于研究骨质疏松症，颅面和阑尾骨骼缺损以及靶向骨再生。

GC61807 (E/Z)-AG490

酪氨酸磷酸化抑制剂AG490,(E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42

(E/Z)-AG490((E/Z)-TyrphostinAG490)是(E)-AG490和(Z)-AG490的消旋体。(E)-AG490是一种酪氨酸激酶抑制剂，可抑制EGFR，Stat-3和JAK2/3。

GC61780 SU5204 SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.

GC61741 GIP, human TFA

抑胃肽三氟乙酸盐 (人); Gastric Inhibitory Peptide (GIP), human TFA

GIP,humanTFA是一种由42个氨基酸组成的肽类激素，是葡萄糖依赖性胰岛素分泌的促进剂和胃酸分泌的弱抑制剂。GIP,humanTFA作为肠K细胞释放的肠促胰岛素激素，对营养摄入作出反应。

GC61600 VEGFR-2-IN-6

帕唑帕尼杂质3

VEGFR-2-IN-6(example64)是VEGFR2的抑制剂(血管生成的调节剂)，信息来自专利WO02/059110的example64。

GC61569 GIP (1-30) amide, porcine TFA GIP(1-30)amide,porcineTFA是一种葡萄糖依赖性促胰岛素多肽(GIP)受体激动剂，与天然GIP(1-42)的亲和力一样高。GIP(1-30)amide,porcine是一种弱的胃酸分泌抑制剂，有效刺激胰岛素分泌。

GC61550 S961 acetate S961acetate是一种高亲和力的胰岛素受体(insulinreceptor,IR)拮抗剂，对HIR-A，HIR-B和人胰岛素样生长因子I受体(HIGF-IR)的IC50分别为0.048，0.027和630nM。

GC61516 MID-1 MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin 53-insulin receptor substrate-1) interaction, which can disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake.

GC61490 Trastuzumab emtansine

曲妥珠单抗-美坦新偶联物; Ado-Trastuzumab emtansine; PRO132365; T-DM 1

Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.

GC61473 Trastuzumab deruxtecan

DS-8201 (solution); DS-8201a (solution)

Trastuzumab deruxtecan（曲妥珠单抗）是一种人表皮生长因子受体2（HER2）靶向抗体-药物偶联物（ADC），由人源化抗人HER2（抗hHER2）抗体、酶促裂解肽接头和拓扑异构酶I抑制剂（DX-8951衍生物）组成。

GC61454 GW806742X hydrochloride GW806742Xhydrochloride是一种ATP模拟物，是一种有效的MLKL抑制剂，结合MLKL假激酶结构域，Kd值为9.3μM。GW806742Xhydrochloride具有抗VEGFR2的活性(IC50=2nM)。GW806742Xhydrochloride延缓MLKL膜移位并抑制坏死。