Tyrosine Kinase

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Cat. No.	Product Name	Field of Application
DC3134	Vandetanib (ZD6474) Featured	Vandetanib (Zactima, ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
DC7607	Vatalanib Featured	Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 1/2.
DC8655	Vatalanib free base	Vatalanib free base (PTK787 free base) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4.
DC11268	VEGFR2 kinase inhibitor I(SU-5408) Featured	VEGFR2 kinase inhibitor I(SU-5408)is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase (IC50 = 70 nM).
DC7657	WH-4-023 Featured	WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
DC7558	WP1130(Degrasyn) Featured	WP1130(Degrasyn) is a novel selective small molecular deubiquitinase (USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and a Bcr/Abl destruction pathway activator with an IC50 of 1.8 μM for K562 cells.
DC10916	WY-135	WY-135 (WY135) is a novel potent inhibitor of ALK and ROS1 with IC50 of 1.2 and 0.48 nM, respectively.
DC9775	WZ3146 Featured	WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).
DC5090	WZ4002 Featured	WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM; does not inhibit ERBB2 phosphorylation (T798I).
DC1097	XL-184 (Cabozantinib,BMS907351) Featured	XL184 (Cabozantinib) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
DC3129	xl647	XL647 is a novel spectrum-selective kinase inhibitor for EGFR, ErbB2, KDR, Flt-4 and EphB4 with IC50 of 0.3 nM, 16 nM, 1.5 nM, 8.7 nM and 1.4 nM, respectively.
DC9941	XMD16-5 Featured	XMD16-5 is a novel TNK2 inhibitor.
DC9940	XMD8-87 Featured	XMD8-87 is a novel TNK2 inhibitor.
DC9446	Y15 Featured	Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.
DC11471	BGB-3111(Zanubrutinib) Featured	Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
DC8871	ZM 323881 HCl	ZM 323881 hydrochloride is a potent and selective inhibitor of human Flk-1 (vascular endothelial growth factor receptor 2, VEGFR-2/KDR) activity.
DC1082	ZM306416 Featured	ZM306416 is a vascular endothelial growth factor receptor (VEGFR) antagonist.
DC1083	ZM323881 hydrochloride	ZM323881 a receptor tyrosine kinase inhibitor of VEGFR-2 (Flk-1), PDGFR-beta, EGFR, and FGFR1
DC10764	Theliatinib (HMPL-309) Featured	Theliatinib (HMPL-309) is a novel small molecule, EGFR tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities.
DC7376	BMS777607 Featured	BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM.
DC7763	NVP-AST487 Featured	AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
DC11089	TAS-120 (Futibatinib) Featured	TAS-120 is a highly potent and selective irreversible FGFR inhibitor, effective in tumors harboring various FGFR gene abnormalities.
DC12371	XL-999(Tyrosine kinase-IN-1) Featured	XL999, a Spectrum Selective Kinase Inhibitor(TM) (SSKIs), is a potent inhibitor of key RTKs implicated in the development and maintenance of tumor vasculature and in the proliferation of some tumor cells.
DC7052	AG-1024 (Tyrphostin) Featured	AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.
DC12161	TAS6417 Featured	TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
DC11689	RU-301 Featured	RU-301 (RU301) is a small molecule pan-TAM inhibitor that targets the TAM Ig1-Gas6 interface, blocks Gas6-dependent TAM activation.
DC11450	Selpercatinib(LOXO-292) Featured	Selpercatinib is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively. Antineoplastic activity.
DC7622	BIBX1382 Featured	BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).
DC28032	EMI1 (EGFR MaMTH Inhibitor 1) Featured	EMI1 (EGFR MaMTH Inhibitor 1) is a novel EGFR ex19del/T790M/C797S inhibitor.EMI1, while potently reducing the interaction of EGFR triple mutant with Shc1 in our MaMTH-DS assay, did not behave as a TKI and displayed no inhibition of the kinase activity of EGFR triple-mutant protein invitro.EMI1 did, however, more strongly inhibit the viability and increase the caspase 3/7 activ-ity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells, as well as potently reduce PC9 EGFR ex19del/T790M/C797S organ-oid viability.EMI1 had a similar inhibi-tory effect on microtubule plus-end growth in both EGFR-WT and EGFR-C797S triple-mutant cells at 50–100 nM concentration. At 1 µM concentration, EMI1 strongly depolymerized inter-phase microtubules, perturbed spindle formation and induced strong mitotic block in PC9 EGFR ex19del/T790M/C797S cells after 20 h of treatment. EMI1 inhibited interaction of both proteins with EGFR at a level similar to that observed with Shc1, indicating it is not a specific inhibitor of the EGFR-Shc1 PPI interface. Rather, the loss of interaction mediated by EMI1 appears to be due to a more general alteration in EGFR activity.EMI1 induced EGFR degradation, and inhibited the activation of EGFR, ERK, AKT and S6 in PC9-ex19del and PC9-ex19del/T790M cells.
DC28069	O-Desmethyl gefitinib	O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays.

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Tyrosine Kinase

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