Crotonoside is one compound of an antitumor and immunity-regulating pharmaceutical composition of traditional Chinese medicine.
Crotonoside inhibits the growth of S-180 and Ehrlich solid tumor in mice at the optimal doses of 96 mg/kg/...
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibitsFMS-like tyrosine kinase-3 (FLT3)autophosphorylation with IC50s of approximately 132nM and 9.8μM in culture medium and plasma, respectivel...
CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.
Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for P...
Gilteritinib(ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent tha...
SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10 nM.
AMG 925 is a potent, selective, and orally availableFLT3/CDK4dual inhibitor with IC50s of 2±1nM and 3±1nM, respectively.
AMG 925 HCl
AMG 925 HCl is a potent, selective, and orally availableFLT3/CDK4dual inhibitor with IC50s of 2±1nM and 3±1nM, respectively.
CCT241736 is a potent and orally bioavailable dualFLT3 and Aurora kinaseinhibitor, which inhibits Aurora kinases (Aurora-AKd, 7.5nM,IC50, 38nM; Aurora-BKd, 48nM), FLT3 kinase (Kd, 6.2nM), and FLT3 mutants incl...
FN-1501 is a potent inhibitor ofFLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.
UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with ...
MRX-2843 (UNC2371) is an orally active dualMERTK and FLT3tyrosine kinases inhibitor (TKI) with enzymaticIC50s of 1.3nM for MERTK and 0.64nM for FLT3, respectively.
G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.
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.
Emavusertib (CA-4948) is a potent and orally bioavailable inhibitor of interleukin-1 receptor-associated kinase 4/FMS-like Tyrosine Kinase 3 (IRAK4/FLT3) with anti-tumor activity.
TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.
UNC2025 hydrochloride is a potent and highly orally activeMer/Flt3inhibitor with IC50 values of 0.74nM and 0.8nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122nM;K...
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