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c-RET
货号 | 产品名 | CAS号 | 信息 |
---|---|---|---|
CSN12405 | Fedratinib | 936091-26-8 | TG 101348 is an inhibitor of JAK2 with an IC₅₀ of 6 nM and also inhibits related kinases FLT3, RET, and JAK3 with less potent activity, having IC₅₀ values of 25, 17 and 169 nM, respectively. |
CSN26200 | SPP-86 | 1357349-91-7 | SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase( IC50 :8 nM). SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells. |
CSN25546 | Selpercatinib | 2152628-33-4 | Selpercatinib is a potent and specific RET inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively. |
CSN26135 | RET V804M-IN-1 | 2414909-94-5 | RETV804M kinase inhibitor is a selective c-RET (V804M) inhibitor with IC50 value of 20nM. |
CSN13099 | Regorafenib | 755037-03-7 | Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13/4.2/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. |
CSN25230 | ODM-203 | 1430723-35-5 | ODM-203 is a selective inhibitor of FGFR and VEGFR with IC50 values of 11, 16, 6, 35nM for recombinant FGFR1-4 and 26, 9, 5nM for VEGFR1-3, respectively. |
CSN23893 | RET-IN-1 | 2222755-14-6 | LOXO-292 is a RET kinase inhibitor with IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively . |
CSN26936 | JNJ-38158471 | 951151-97-6 | JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively . |
CSN24470 | GSK3179106 | 1627856-64-7 | GSK3179106 is a potent, selective and gut-restricted RET kinase inhibitor with IC50 value of 0.4nM. |
CSN27527 | Fedratinib hydrochloride hydrate | 1374744-69-0 | Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research. |
CSN27593 | DUN73423 | 2414373-42-3 | DUN73423 is a RET/KDR-Selective inhibitor of RETV804M Kinase with IC50 of 7 nM. |
CSN12423 | Danusertib | 827318-97-8 | Danusertib is a pyrrolo-pyrazole and small molecule Aurora kinases inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively. It is modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. |
CSN15883 | Agerafenib | 1188910-76-0 | CEP-32496 is an inhibitor of BRAF V600E (IC50 = 14 nM), WT (IC50 = 34 nM) and c-Raf (IC50 = 39 nM). It also exhibits certain inhibitory activity against Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2. |
CSN28779 | BT-13 | 924537-98-4 | BT13 acts as direct RetA agonists and interacts with GFRα1 at the allosteric site in GDNF-GFRα1-RetA complex. It was similar to NGF and ARTN in selectively promoting neurite outgrowth from the peptidergic class of adult sensory neurons in culture, but was opposite to ARTN in causing neurite elongation without affecting initiation. |
CSN22922 | Pralsetinib | 2097132-94-8 | Blu667 is a highly potent and selective RET inhibitor with IC50 value of 0.4nM. |
CSN18365 | AST 487 | 630124-46-8 | AST-487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM. AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. |
CSN22316 | AD80 | 1384071-99-1 | AD80 is a multikinase inhibitor with inhibitions on RET, RAF, SRC and S6K. |