Catalog |
name |
Description |
price |
R-C-1322 |
Brigatinib (AP26113) CAS:1197953-54-0 |
Brigatinib,also known as AP-26113,is an orally active,potent and selective Dual ALK/EGFR inhibitor.AP26113 binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms.This leads to the inhibition of ALK kinase and EGFR kinase,disrupts their signaling pathways and eventually inhibits tumor cell growth in susceptible tumor cells.In addition,AP26113 appears to overcome mutation-based resistance.ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development;ALK dysregulation and gene rearrangements are associated with a series of tumors. EGFR is overexpressed in a variety of cancer cell types. |
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R-C-1347 |
R-112 CAS: 575474-82-7 |
R112 is a Syk inhibitor.R112 inhibited degranulation induced by anti-IgE cross-linking in mast cells(tryptase release,effective concentration for 50% inhibition[EC(50)]=353 nmol/L)or basophils(histamine release,EC(50)=280 nmol/L),and by allergen(dust mite)in basophils(histamine release,EC(50)=490 nmol/L). |
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R-C-1371 |
GNF-7 CAS:839706-07-9 |
GNF-7 is a multikinase inhibitor.GNF-7 is a Bcr-Abl inhibitor,with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I,respectively.GNF-7 also possesses inhibitory activity against both ACK1(activated CDC42 kinase 1) and GCK(germinal center kinase)with IC50s of 25 nM and 8 nM,respectively.GNF-7 can be used for the research of hematologic malignancies. |
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R-C-1373 |
GZD824 CAS:1257628-77-5 |
Olverembatinib,also known as GZD824,is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I.GZD824 tightly bound to Bcr-Abl(WT)and Bcr-Abl(T315I)with K(d)values of 0.32 and 0.71 nM, respectively,and strongly inhibited the kinase functions with nanomolar IC(50) values.GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50)values of 0.2 and 0.13 nM, respectively.GZD824 also displayed good oral bioavailability (48.7%),a reasonable half-life(10.6h), and promising in vivo antitumor efficacy.It induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT)or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I).GZD824 represents a promising lead candidate for development of Bcr-Abl inhibitors to overcome acquired imatinib resistance.(J Med Chem.2013 Feb 14;56(3):879-94). |
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R-C-1378 |
BLU-554 CAS:1707289-21-1 |
Fisogatinib,also known as BLU-554,is a fibroblast growth factor receptor 4 (FGFR4)inhibitor potentially for the treatment of hepatocellular carcinoma and cholangiocarcinoma.Fisogatinib demonstrates clinical benefit and tumor regression in patients with HCC with aberrant FGF19 expression. |
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R-C-1406 |
PP1 CAS: 172889-26-8 |
PP1 is a potent inhibitor of Src-family tyrosine kinases.Inhibits p56lck and p59fynT(IC50 values are 5 and 6 nM respectively).Display>8000-fold selectivity over ZAP-70 and JAK2.Also moderately inhibits p38,CSK,PDGF receptors,RET-derived oncoproteins,c-Kit and Bcr-Abl. |
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R-C-1420 |
HM71224 CAS :1353552-97-2 |
Poseltinib,an orally active,selective and irreversible Bruton? is tyrosine kinase (BTK)inhibitor(IC50=1.95 nM),with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX,TEC and TXK,respectively. |
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R-C-1451 |
KC7F2 CAS:927822-86-4 |
KC7F2 is an inhibitor of HIF-1αprotein translation,but not transcription,that suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1(4EBP1)and p70 S6 kinase(S6K). |
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R-C-1483 |
Verteporfin (CL 318952) CAS:129497-78-5 |
Verteporfin(CL 318952,Visudyne)is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth.It is also a potent second-generation photosensitizing agent derived from porphyrin.Verteporfin is an autophagy inhibitor.Verteporfin inhibits cell proliferation and induces apoptosis. |
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R-C-1501 |
nsc12 CAS:102586-30-1 |
NSC-12(NSC 172285)is an extracellular FGF trap with significant implications in cancer therapy.NSC12 inhibited the proliferation of different FGF-dependent tumour cell lines,but had no inhibitory effect on FGF-independent tumour cells expressing a constitutively active FGFR1.NSC12 was shown to inhibit FGFR phosphorylation,angiogenesis and primary and metastatic tumour growth of FGF-dependent human and mouse cancer cells.Importantly,there was no systemic toxic effect. |
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