Tyrosine Kinase(酪氨酸激酶)

Cat.No. 产品名称 Information

GC32979 Chloropyramine hydrochloride

盐酸氯吡胺

Chloropyramine hydrochloride (Halopyramine) is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.

GC32968 FLT3-IN-1 FF-10101 is a novel irreversible FLT3 inhibitor with ic50 of 0.20 nM and 0.16 nM for FLT3 (WT) and FLT3(D835Y), respectively.

GC32963 hVEGF-IN-1 hVEGF-IN-1, a quinazoline derivative, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) with a Kd of 0.928 μM, therefore destabilizes the G-quadruplex structure, , also hinders tumor cells migration and represses tumor growth by decreasing VEGF-A protein expression.

GC32927 PF-06459988 PF-06459988是T790M-ContainingEGFRMutants不可逆性抑制剂。

GC32915 Pemigatinib

培米加替尼,INCB054828

An FGFR inhibitor

GC32875 AZM475271 (M475271)

M475271

An inhibitor of c-Src kinase

GC32867 Flumatinib (HHGV678)

4-[(4-甲基-1-哌嗪基)甲基]-N-[6-甲基-5-[[4-(3-吡啶基)-2-嘧啶基]氨基]-3-吡啶基]-3-(三氟甲基)苯甲酰胺,HHGV678

A Bcr-Abl inhibitor

GC32864 Ensartinib hydrochloride (X-396 hydrochloride)

X-396 dihydrochloride

An ALK inhibitor

GC32836 Naquotinib mesylate (ASP8273)

ASP8273 (mesylate)

An irreversible inhibitor of mutant EGFRs

GC32835 PP58

PP58是吡啶[2,3-d]嘧啶化合物，抑制PDGFR，FGFR和Src家族活性的IC50值在纳摩尔级。

GC32825 eCF506 An inhibitor of Src kinases

GC32819 Mirk-IN-1 (Dyrk1B/A-IN-1)

Dyrk1B/A-IN-1

Mirk-IN-1 (Dyrk1B/A-IN-1) 是一种有效的 Dyrk1B(Mirk kianse) 和 Dyrk1A 抑制剂，IC50 分别为 68±48 nM 和 22±8 nM。

GC32808 Selitrectinib (LOXO-195)

LOXO-195

A Trk kinase inhibitor

GC32805 Sulfatinib (HMPL-012)

5-羟基-2-甲基吲哚,HMPL-012

A multi-kinase inhibitor

GC32802 PRN1371 An irreversible pan-FGFR inhibitor

GC32797 AD80 AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.

GC32769 MRX-2843 (UNC2371)

UNC2371

A Mer and FLT3 inhibitor

GC32760 Dovitinib lactate (CHIR-258 lactate)

多韦替尼乳酸盐; CHIR-258 lactate; TKI-258 lactate

A multi-kinase inhibitor

GC32752 TAS6417

TAS6417; CLN-081

TAS6417 (CLN-081, TPC-064) is a novel EGFR inhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L.

GC32748 CA-4948 An IRAK-4 inhibitor

GC32733 Pyrotinib (SHR-1258)

吡咯替尼; SHR-1258

Pyrotinib (SHR-1258) (SHR-1258) 是一种有效的选择性 EGFR/HER2 双重抑制剂，IC50 分别为 13 和 38 nM。

GC32731 OSU-T315 (ILK-IN-1)

OSU-T315 analog

An ILK inhibitor

GC32726 Tucatinib (Irbinitinib)

妥卡替尼,Irbinitinib; ARRY-380; ONT-380

An inhibitor of HER2

GC32713 Cintirorgon (LYC-55716)

LYC-55716

A ROR? agonist

GC32703 Asciminib (ABL001)

ABL001

An allosteric inhibitor of Abl1

GC32625 KDR-in-4

KDR-in-4

KDR-in-4 (KDR-in-4) 是一种有效的激酶插入结构域受体 (KDR/VEGFR2) 抑制剂，IC50 为 7 nM。

GC32623 CE-245677 CE-245677是一种有效的，可逆的Tie2和TrkA/B抑制剂，在细胞体系下，IC50值分别为4.7和1nM。

GC32502 Oglufanide (H-Glu-Trp-OH)

奥谷法奈; H-Glu-Trp-OH; L-Glutamyl-L-tryptophan

Oglufanide (H-Glu-Trp-OH) (H-Glu-Trp-OH) 是一种从小牛胸腺中分离出来的二肽免疫调节剂。

GC32469 SU5408 (VEGFR2 Kinase Inhibitor I)

VEGFR2 Kinase Inhibitor I

A potent, cell-permeable inhibitor of VEGFR2

GC32458 Trapidil (AR-12008)

唑嘧胺; AR-12008

An inhibitor of PDGF-induced activity and an antiplatelet agent

GC19772 FLT3-IN-3

SAN50900

An FLT3 inhibitor

GC32127 Alofanib (RPT835)

RPT835

An allosteric inhibitor of FGFR2

GC32100 Tarloxotinib bromide (TH-4000)

TH-4000

Tarloxotinib bromide (TH-4000)是一种不可逆的EGFR/HER2抑制剂前体。

GC32053 GNE-4997 GNE-4997是一种有效且有选择性的ITK/TSK抑制剂。

GC32044 L 601920-0 (Methyl-3β-hydroxycholenate)

5-胆烯-24-酸-3Β-醇甲酯

L 601920-0 (Methyl-3β-hydroxycholenate) 是一种从专利 US20110263046 A1 中提取的 ROR γ 调节剂，如图 2 所示。

GC31880 AZD-0284 AZD-0284是核受体RORγ的反向激动剂。在开发用于治疗寻常型斑块状银屑病和呼吸道疾病。

GC31871 GNE-0946 GNE-0946是一个有效且有选择性的RORγ(RORc)拮抗剂，对HEK-293细胞的EC50值为4nM.

GC31842 GENZ-882706 (RA03546849)

RA03546849

GENZ-882706 (RA03546849) 是一种有效的集落刺激因子-1 受体 (CSF-1R) 抑制剂，提取自专利 WO 2017015267A1。

GC31819 PRT062607 (P505-15)

2-[[(1R,2S)-2-氨基环己基]氨基]-4-[[3-(2H-1,2,3-三唑-2-基)苯基]氨基]-5-嘧啶甲酰胺,P505-15; PRT-2607; BIIB-057

A potent, orally bioavailable Syk inhibitor

GC31816 ZK-261991 ZK-261991是一种可口服的VEGFR酪氨酸酶抑制剂，抑制VEGFR-2活性的IC50值为5nM。

GC31780 Pralsetinib (Blu667)

普拉替尼; BLU-667

Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).