Tyrosine Kinase(酪氨酸激酶)

Cat.No. 产品名称 Information

GC50026 BIBX 1382 dihydrochloride An EGFR inhibitor

GC50024 Caffeic acid-pYEEIE 咖啡酸-pYEEIE 是一种非磷酸肽抑制剂，对 GST-Lck-SH2 结构域具有强大的结合亲和力。

GC50013 AG 1478 hydrochloride

N-(3-氯苯基)-6,7-二甲氧基-4-喹唑啉胺盐酸盐,Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride

An inhibitor of EGF receptor kinase

GC39314 Tyrphostin AG1433

SU1433; AG1433

Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively.

GC39301 VU6015929 VU6015929 is a selective Discoidin Domain Receptor 1/2 (DDR1/2) inhibitor with IC50 of 4.67 nM and 7.39 nM for DDR1 and DDR2, respectively. VU6015929 potently inhibits collagen-IV production.

GC39299 TMP920 TMP920 是一个高效、选择性的 RORγt 拮抗剂。TMP920 抑制 RORγt 结合 SRC1 肽的 IC50 值为 0.03 μM。

GC46208 Propentofylline

普罗潘非林,HWA 285

A xanthine derivative and neuroprotective agent

GC46197 PD 90780 (hydrate) An inhibitor of NGF-p75 NGFR interactions

GC46123 Comprehensive Kinase Screening Library For screening of a variety of kinase inhibitors

GC39189 S961 TFA S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.

GC38894 Bozitinib

PLB-1001; CBT-101; Vebreltinib

Bozitinib (PLB-1001, CBT-101, APL-101, CBI-3103) is a highly selective ATP-competitive c-Met inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) selectively inhibits MET-altered tumor cells in preclinical models.

GC46013 AS-2444697 (hydrochloride) An IRAK4 inhibitor

GC38864 TL02-59 TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM.

GC38853 Tandutinib hydrochloride

MLN518 hydrochloride; CT53518 hydrochloride

An antagonist of PDGFRβ, FLT3, and c-Kit

GC38836 PLX5622 hemifumarate A CSF1R inhibitor

GC38799 IRAK4-IN-4 IRAK4-IN-4 (compound 15) is an inhibitor of interleukin-1 receptor–associated kinase 4 (IRAK4) and cyclic GMP-AMP synthase (cGAS) with IC50 of 2.8 nM and 2.1 nM, respectively.

GC38787 GNF4877 GNF4877是 DYRK1A 和 GSK3β 的有效抑制剂，IC50 值分别为 6 nM 和 16 nM，可导致 NFATc 核输出受阻并增加 β 细胞增殖 (对小鼠 β (R7T1) 细胞的 EC50 值为 0.66 μM)。

GC38776 Ensulizole

苯基苯丙咪唑磺酸

Ensulizole (PBSA), a water soluble sunscreen ingredient, is a sulfonated UV absorber which is characterized by intense UVB and partial UVA absorption. Ensulizole can damage the DNA through the generation of reactive oxygen species (ROS) upon UV or sunlight irradiation.

GC38757 c-Kit-IN-3 hydrochloride c-Kit-IN-3 hydrochloride (Compound 18) 是一种有效的 c-KIT 激酶抑制剂，对 BaF3-tel-c-KIT (IC50 为 4 nM) 和广泛的耐药性突变体 (对 BaF3-tel-c-KIT-T670I 的 IC50 为 8 nM)，具有很高的生物利用度。

GC38756 c-Kit-IN-3 D-tartrate c-Kit-IN-3 (D-tartrate) (Compound 18) 是一种有效的 c-KIT kinase 激酶抑制剂，对 BaF3-tel-c-KIT (IC50 为 4 nM) 和广泛的耐药性突变体 (对 BaF3-tel-c-KIT-T670I 的IC50为 8 nM)，具有很高的生物利用度。

GC45831 SRI-011381 A TGF-β signaling activator

GC45828 Ponatinib-d8

纳替尼-D8,AP24534-d8

An internal standard for the quantification of ponatinib

GC45789 Ceritinib-d7

色瑞替你-D7,LDK378 D7

An internal standard for the quantification of ceritinib

GC45769 Vandetanib-d6

ZD6474-d6

An internal standard for the quantification of vandetanib

GC45767 Dovitinib-d8

多韦替尼 D8

An internal standard for the quantification of dovitinib

GC45754 Lenvatinib-d4

E7080-d4

Lenvatinib-d4 (E7080-d4) 是氘标记的 Lenvatinib。 Lenvatinib (E7080) 是一种口服的多靶点酪氨酸激酶抑制剂，可抑制 VEGFR1-3、FGFR1-4、PDGFR、KIT 和 RET，显示出有效的抗肿瘤活性。

GC45687 Dasatinib N-oxide

达沙替尼N氧化物；达沙替尼杂质

A major metabolite of dasatinib

GC38630 Lanraplenib succinate

GS-9876 succinate

A Syk inhibitor

GC38595 c-Kit-IN-3 c-Kit-IN-3 (Compound 18) 是一种有效的 c-KIT 激酶抑制剂，IC50 为 4 nM。c-Kit-IN-3 在生化分析中显示出对 c-KIT 激酶和多种耐药突变体的强大效价，并具有很高的生物利用度。

GC38580 RU-301 RU-301 is a pan-TAM receptor (Axl, Tyro3 and Mertk) inhibitor that blocks the Axl receptor dimerization site with Kd of 12 μM and IC50 of 10 μM, respectively.

GC38575 CP-547632 hydrochloride A potent inhibitor of VEGFR2 and bFGF

GC38519 Ilorasertib hydrochloride

ABT-348 hydrochloride

A multi-kinase inhibitor

GC38437 Fangchinoline

防己诺林碱

An alkaloid with diverse biological activities

GC38413 Harmine hydrochloride

哈尔碱盐酸盐(水合),Telepathine hydrochloride

A unique regulator of PPARγ expression

GC38412 Crotonoside

巴豆苷; Isoguanosine

Crotonoside是一种FLT3和HDAC3/6抑制剂，可用于研究急性髓系白血病(AML)。

GC38402 BI-4020 BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFRdel19 T790M C797S as biomarker potency and anti-proliferation potency in BaF3 cells, respectively.

GC38380 Vorolanib

CM082; X-82

Vorolanib（X-82；CM082）是一种具口服活性的血管内皮生长因子受体（VEGFR）和血小板衍生生长因子受体（PDGFR）的多激酶双重抑制剂，IC₅₀值分别为0.052μM、0.26 μM。

GC38350 Epertinib hydrochloride

S-22611 hydrochloride

Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.

GC38330 EHT 5372 EHT 5372 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂，其 IC50 值分别为 0.22，0.28 nM。

GC38206 WRG-28 WRG-28 是选择性，细胞外作用的 DDR2 变构抑制剂，IC50 为 230 nM。WRG-28 通过受体的变构调节特异地抑制受体-配体相互作用。WRG-28 通过靶向 DDR2 抑制肿瘤侵袭和迁移，基质的肿瘤支持作用，并抑制肺中的转移性乳腺肿瘤细胞定植。

GC38180 Cyasterone

杯苋甾酮

Cyasterone，一种天然的 EGFR 抑制剂，主要分离自 Ajuga decumbens Thunb (Labiatae)。Cyasterone 通过诱导细胞凋亡 (apoptosis) 和细胞周期阻滞表现出抗增殖作用。 Cyasterone 可作为抗人类肿瘤的临床治疗性药物。

GC38125 Tyrphostin AG30

酪氨酸磷酸化抑制剂AG30,AG30

Tyrphostin AG30 (AG30), a potent and selective EGFR tyrosine kinase inhibitor, selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.

GC38081 Theliatinib

西利替尼; Xiliertinib; HMPL-309

Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.

GA23328 Osteogenic Growth Peptide (10-14)

OGP(10-14); Historphin

成骨生长肽 (10-14) (OGP(10-14)) 是成骨生长肽 (OGP) 的 C 末端截短的五肽，保留了完整的 OGP 样活性。

GA21894 Gastric Inhibitory Polypeptide (3-42) (human) Gastric Inhibitory Polypeptide (3-42) (human) 作为葡萄糖依赖性促胰岛素多肽 (GIP) 受体拮抗剂，在体内调节 GIP 的胰岛素分泌和代谢作用。

GA21893 Gastric Inhibitory Polypeptide (1-30) amide (porcine) Gastric Inhibitory Polypeptide (1-30) amide (porcine) 是一种完全依赖葡萄糖的促胰岛素多肽 (GIP) 受体激动剂，具有与天然 GIP(1-42) 相同的高亲和力。

GC38006 β-Hydroxyisovalerylshikonin

β-羟基异戊酰基紫草素

Beta-hydroxyisovalerylshikonin 是一种从Lithospermium radix 中分离出的天然产物，是一种有效的 PTK 抑制剂，对 EGFR 和 v-Src 受体作用的 IC50 分别为 0.7 μM 和 1 μM。Beta-hydroxyisovalerylshikonin 对多种肿瘤细胞系均有抑制作用，能高效诱导 NCI-H522 和 DMS114 细胞的死亡。

GC37944 XY101 XY101 是一种有效选择性的、代谢稳定的口服 RORγ 反向激动剂，IC50 为 30 nM，Kd 为 380 nM。

GC37933 WHI-P180 hydrochloride

Janex 3 hydrochloride;

A multi-kinase inhibitor

GC37886 Vandetanib trifluoroacetate

凡德他尼,ZD6474 trifluoroacetate

A multi-kinase inhibitor