| DC74395 |
ER121 |
ER121 (ER-121) is a potent, dual kinase inhibitor targeting both mutant EGFR and activated erbB2 with IC50 of 0.08/0.15 nM (EGFR C797S/EGFR WT, ATP=10 uM). |
|
| DC74396 |
HCD3514 |
HCD3514 is a novel potent, selective, fourth-generation EGFR inhibitor targeting C797S triple mutation, strongly inhibits EGFRL858R/T790M/C797S and EGFR19del/T790M/C797S mutations with IC50 of 1.0 and 2.0 nM, respectively. |
|
| DC74397 |
HNPMI |
HNPMI is a small molecule inhibitor of epidermal growth factor receptor (EGFR) with the anticancer potential against various cancers. |
|
| DC74398 |
HSL119
Featured
|
HSL119 is a highly effective and selective inhibitor of hormonally upregulated neu-associated kinase (HUNK), demonstrating complete suppression of HUNK kinase activity at a concentration of 1 µM in biochemical assays. This compound highlights its precision and potency in targeting HUNK.
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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. |
|
| DC74400 |
OBX02-011
Featured
|
OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively. |
|
| 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. |
|
| DC74402 |
STX-721 |
STX-721 is a potent, selective, next-generation, orally active inhibitor of EGFR exon 20 insertion mutations. |
|
| 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. |
|
| DC74404 |
TAS2940 |
TAS2940 (TAS-2940) is a potent, selective, orally active, irreversible and brain-penetrable pan-ERBB inhibitor. |
|
| 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. |
|
| DC74406 |
WCDD301 |
WCDD301 is a high-affinity, orally available agonist of EphA4 receptor. |
|
| DC74407 |
ABSK011 |
Irpagratinib (ABSK011) is a potent, selective FGFR4 inhibitor with strong antitumor activity against hepatocellular carcinoma (HCC). |
|
| 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. |
|
| 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. |
|
| 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). |
|
| 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. |
|
| 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. |
|
| 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). |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC74422 |
BI 1342561 |
BI 1342561 is a novel potent and selective SYK inhibitor developed to treat severe asthma. |
|
| DC74423 |
BI 894416 |
BI 894416 is a novel potent and selective SYK inhibitor developed to treat severe asthma. |
|
| 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). |
|
| 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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