| DC74386 |
Leucettinib-21 |
Leucettinib-21 is a potent, selective DYRKs and CLKs kinases with IC50 of 2.4, 6.7, 12, 33, and 5 nM for DYRK1A, DYRK1B, CLK1, CLK2, and CLK4, respectively. |
|
| DC74387 |
Y020-3945 |
Y020-3945 is a selective dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor with IC50 of 0.53 uM. |
|
| DC74388 |
YK-2-69 |
YK-2-69 is a potent, hilghly selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with IC50 value of 9 nM, shows weak inhibition against DYRK1B (IC50=542 nM) and no activity against DYRK1A/3/4 (IC50>1,000 nM). |
|
| DC74389 |
ARRY-380 analog |
An analog of ARRY-380, a potent and selective HER2 inhibitor with IC50 of 8 nM. |
|
| DC74390 |
AZD-9291 dimesylate |
A potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively. |
|
| DC74391 |
BI-1622 |
BI-1622 (BI 1622) is a potent, selective, covalent and orally active HER2 inhibitor with IC50 of 7 nM, potently inhibits HER2 exon 20 mutants while sparing WT EGFR. |
|
| DC74392 |
BI-4732 |
BI-4732 is a potent, highly BBB penetrant, fourth-generation EGFR inhibitor against EGFR activating mutations, including C797S. |
|
| DC74393 |
BI-8128 |
BI-8128 is a potent, selective, reversible and orally bioavailable fourth generation EGFR inhibitor, potently inhibits oncogenic EGFR variants del19 and L858R as well as the acquired EGFR resistance mutations T790M and C797S. |
|
| DC74394 |
DSF-102
Featured
|
DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of |
|
| 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.
|
|
| 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. |
|
