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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC74429 ER-851
ER851 (ER-851) is a potent and highly selective AXL inhibitor.
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DC74428 Adrixetinib
Adrixetinib is a small molecule inhibitor of Axl/Mer RTK.
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DC74427 RDN2150
RDN2150 is a potent, selective and covalent ZAP-70 inhibitor with IC50 of 14.6 nM, shows no significant activity against Syk, covalently binds to the C346 residue of ZAP-70.
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DC74426 RDN009
RDN009 (RDN-009) is a potent, selective, and covalent ZAP-70 kinase inhibitor with IC50 of 55 nM.
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DC74425 MTX-216
MTX-216 (MTX216) is a dual PI3K/EGFR inhibitor that blocks neurofibromin 1 loss of function (NF1LoF) melanoma cell growth in vitro and in vivo, suppresses the activity of SYK kinase with IC50 of 281 nM.
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DC74424 MRL-SYKi
MRL-SYKi is a potent, selective inhibitor of Syk (Spleen tyrosine kinase) with IC50 of <100 nM, also potently inhibits ZAP70 (24 nM in vitro).
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DC74423 BI 894416
BI 894416 is a novel potent and selective SYK inhibitor developed to treat severe asthma.
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DC74422 BI 1342561
BI 1342561 is a novel potent and selective SYK inhibitor developed to treat severe asthma.
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DC74421 TG 100801
The prodrug of TG 100572, a potent, dual receptor tyrosine kinase/Src kinase inhibitor with IC50 of 2-16 nM for VEGFR, FGFR and PDGFR, 0.1-5 nM for Src family.
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DC74420 HSN608
HSN608 (HSN 608) is a potent inhibitor of RET solvent-front mutants, inhibits RET G810 solvent-front mutants and the V804M gatekeeper mutant with IC50 of <50 nM in cell culture, inhibits ABL1(T315I) with IC50 of 40.7 nM.
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DC74419 JTE-051
JTE-051 (JTE051) is a potent, selective inhibitor of interleukin-2-inducible T cell kinase (ITK), suppresses overactive immune response via inhibition of the signal to activate T cells related to immune response.
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DC74418 GNE-4997
GNE-4997 is a potent and selective inhibitor of the interleukin-2-inducible T-cell kinase (ITK) with Ki of 0.09 nM.
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DC74417 GTX-134
GTx-134 (GTx 134) is a selective small-molecule inhibitor of IGF-1R and insulin receptor (IR) with biochemical IC50 of 97 nM and 187 nM, respectively.
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DC74416 BM001
BM001 (BM-001) is a small molecular inhibitor of the integral growth hormone/insulin-like growth factor-1 (GH/IGF1) axis, shows potent antiproliferative effect on cancer cells MDA-MM-231 and Colo-205 with IC50 of 20-30 nM.
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DC74414 BSJ-04-175
BSJ-04-175 is a potent, selective focal adhesion kinase (FAK, protein tyrosine kinase 2 or PTK2) inhibitor with biochemical IC50 of 22 nM, 30-fold selectivity over PYK2.
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DC74413 YHJ1039
YHJ1039 is a broad-spectrum kinase inhibitor, possesses excellent potencies against FLT3 mutants (FLT3 D835Y, IC50=0.41 nM) as well as FAK (IC50=7 nM).
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DC74412 TSN084
TSN084 (TSN 084) is a unique small molecule multi-kinase inhibitor of drug-resistant mutations of c-Met, Trks, and Flt3, also inhibits other oncotargets including Axl, DDRs, and CDK8/19.
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DC74411 PCW-A1001
PCW-A1001 is a potent, selective inhibitor of FLT-3 (D835Y) mutant with IC50 of 764 nM, weakly inhibits WT FLT-3 with IC50 of 2.54 uM.
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DC74410 MBP-11901
MBP-11901 is an orally active, multitarget tyrosine kinase inhibitor targeting FLT3, VEGFR2, PDGFRβ, and c-KIT, shows excellent inhibitory activity against HCC cell growth in vitro (HepG2, IC50=5.16 uM).
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DC74409 Danatinib
Danatinib is a potent and selective FLT3 inhibitor with IC50 of 3 nM, overcomes acquired resistance and shows effective inhibition against FLT3-ITD and/or FLT3-TKD mutations.
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DC74408 DW14383
DW14383 is a potent, selective and irreversible inhibitor of FGFR1-4 with IC50 of <0.3 nM, 1.1 nM, <0.3 nM and 0.5 nM for FGFR1/2/3/4 respectively.
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DC74407 ABSK011
Irpagratinib (ABSK011) is a potent, selective FGFR4 inhibitor with strong antitumor activity against hepatocellular carcinoma (HCC).
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DC74406 WCDD301
WCDD301 is a high-affinity, orally available agonist of EphA4 receptor.
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DC74405 Targefrin
Targefrin is a potent, selective antagonist targeting ligand binding domain of receptor tyrosine kinase EphA2 (EphA2-LBD), binds to EphA2-LBD with Kd of 21 nM (ITC) and shows IC50 value of 10.8 nM in biochemical assays.
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DC74404 TAS2940
TAS2940 (TAS-2940) is a potent, selective, orally active, irreversible and brain-penetrable pan-ERBB inhibitor.
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DC74403 TAS-121
TAS-121 (TAS 121) is an orally available, potent, novel third-generation EGFR-TKI that selectively targets EGFR activating and T790M resistance mutations, sparing wild-type EGFR.
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DC74402 STX-721
STX-721 is a potent, selective, next-generation, orally active inhibitor of EGFR exon 20 insertion mutations.
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DC74401 SDT-011
SDT-011 (SDT011) is a small molecule that effectively blocks the binding of anti-EGFR monoclonal antibodies to EGFR, blocks cetuximab-EGFR binding by 62% at 10 uM, binds to EGFR with Kd of 1.7 nM in MST assays.
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DC74399 MTX-241F
MTX-241F (MTX241F) is a potent, highly selective and brain-penetrant inhibitor of EGFR, PI3K and DNA-PK with IC50 of 3 nM, 87 nM (PI3Kα) and 5.5 nM, respectively.
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DC74397 HNPMI
HNPMI is a small molecule inhibitor of epidermal growth factor receptor (EGFR) with the anticancer potential against various cancers.
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