Tyrosine Kinase(酪氨酸激酶)

Cat.No. 产品名称 Information

GC33181 T338C Src-IN-2

T338CSrc-IN-2是突变型c-Src激酶抑制剂，IC50值317nM，还能抑制T338C/V323A和T338C/V323S双突变Src活性，IC50值57和19nM。

GC33173 TAS-115

TAS-115

A multi-kinase inhibitor

GC33172 BGB-102 (JNJ-26483327)

17-溴-1,8,9,10,11,12,13,14-八氢-20-甲氧基-13-甲基-4,6-乙烯桥嘧啶并[4,5-B][6,1,12]苯并氧杂二氮杂环十五碳七烯,JNJ-26483327

BGB-102 (JNJ-26483327) 是一种有效的多激酶抑制剂，针对 EGFR、HER2 和 HER4，IC50 分别为 9.6 nM、18 nM 和 40.3 nM。

GC33171 ZD-4190 ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.

GC33168 T338C Src-IN-1 T338CSrc-IN-1是突变型c-SrcT338C高效抑制剂，IC50值111nM。对WTSrc活性弱10倍以上。

GC33141 SKLB4771 (FLT3-IN-1)

FLT3-?IN-?1

SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10?nM.

GC33131 NRC-2694 NRC-2694是一种表皮生长因子受体(EGFR)拮抗剂，具有抗癌、抗增殖的活性。

GC33112 CH7057288 CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.

GC33096 AST2818 mesylate

甲磺酸伏美替尼; Furmonertinib mesylate; AST2818 mesylate

An inhibitor of mutant EGFRs

GC33090 AZ-23 (AZ23)

5-氯-N-[(1S)-1-(5-氟吡啶-2-基)乙基]-N'-(5-异丙氧基-1H-吡唑-3-基)嘧啶-2,4-二胺,AZ23; AZ 23

AZ-23 (AZ23) 是一种 ATP 竞争性和口服生物可利用的 Trk 激酶 A/B/C 抑制剂，IC50 为 2 nM (TrkA)、8 nM (TrkB)、24 nM (FGFR1)、52 nM (Flt3)、55分别为 nM (Ret)、84 nM (MuSk)、99 nM (Lck)。

GC33087 2,4-Pyrimidinediamine with linker

N2-[4-[(3-氨基丙基)氨基]苯基]-N4-(5-环丙基-1H-吡唑-3-基)-2,4-嘧啶二胺

A multi-kinase inhibitor

GC33086 LDN-192960

3-[(2,7-二甲氧基吖啶-9-基)硫基]丙胺

An inhibitor of haspin and DYRK2

GC33072 AZ7550 An active metabolite of AZ 9291

GC33064 CG-806 (Luxeptinib)

CG-806

CG-806 (Luxeptinib) (CG-806) 是一种具有口服活性、可逆、一流、非共价且有效的 pan-FLT3/pan-BTK 抑制剂。 CG-806 (Luxeptinib) 在急性髓性白血病细胞中诱导细胞周期停滞、凋亡或自噬。

GC33062 JH-VIII-157-02 JH-VIII-157-02是alectinib的结构类似物，为ALK抑制剂，对棘皮动物微管相关蛋白样4(EML4)-ALKG1202R的IC50值为2nM。

GC33061 Rociletinib hydrobromide (CO-1686 (hydrobromide))

CO-1686氢溴酸盐,CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide

Rociletinib hydrobromide (CO-1686 (hydrobromide)) (CO-1686 hydrobromide) 是一种口服激酶抑制剂，特异性靶向 EGFR 的突变形式，包括 T790M，EGFRL858R/T790M 和 EGFRWT 的 Ki 值为 21.5 nM 和 303.3 nM，分别。

GC33054 AZ1495 AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively.

GC33053 HS-10296 hydrochloride

盐酸阿美替尼; HS-10296 hydrochloride

Almonertinib (HS-10296) hydrochloride 是一种口服的、不可逆的第三代 EGFR 酪氨酸激酶抑制剂，对 EGFR 致敏和 T790M 耐药突变具有高选择性。 HS-10296 hydrochloride 对 T790M、T790M/L858R 和 T790M/Del19 具有很强的抑制活性（IC50 分别为 0.37、0.29 和 0.21 nM），而对野生型的抑制效果较差（3.39 nM）。 HS-10296 hydrochloride 用于非小细胞肺癌的研究。

GC33049 FN-1501 FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (CDK), with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively.

GC33048 Epertinib (S-22611)

艾培替尼,S-22611

Epertinib (S-22611) (S-22611) 是一种有效的、口服的、可逆的、选择性的 EGFR、HER2 和 HER4 酪氨酸激酶抑制剂，IC50 分别为 1.48 nM、7.15 nM 和 2.49 nM。 Epertinib (S-22611) 显示出有效的抗肿瘤活性。

GC33045 NAMI-A NAMI-A是一种钌基试剂，其特征在于对肿瘤转移的选择性活性，抑制粘附和迁移。

GC33041 Gusacitinib (ASN-002)

ASN-002

A dual inhibitor of JAKs and Syk family kinases

GC33027 AZD3229 An inhibitor of c-Kit-driven cell proliferation

GC33022 Naquotinib (ASP8273)

ASP8273

An irreversible inhibitor of mutant EGFRs

GC33020 CHMFL-BMX-078 (CHMFL-BMX 078)

CHMFL-BMX 078

An irreversible BMX inhibitor

GC33004 Cediranib maleate (AZD-2171 maleate)

西地尼布马来酸盐; AZD-2171 maleate

An inhibitor of VEGF receptor tyrosine kinases

GC32995 JNJ-47117096 hydrochloride (MELK-T1 hydrochloride)

MELK-T1 hydrochloride

JNJ-47117096 hydrochloride (MELK-T1 hydrochloride) 是有效的选择性 MELK 抑制剂，IC50 为 23 nM，也有效抑制 Flt3，IC50 为 18 nM。

GC32992 7-Hydroxy-4-chromone (7-Hydroxychromone)

7-羟基色原酮,7-Hydroxychromone

7-Hydroxychromone is an inhibitor of Src kinase with IC50 of <300 μM.

GC32989 Pyrotinib dimaleate (SHR-1258 dimaleate)

马来酸吡咯替尼,SHR-1258 dimaleate

Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.

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。