FLT3

下级目录

NameC

SGI-1776 free base

SIM010603

SU-5614

KRC-108

AKN-028

BPR1J-097

BPR1J-340

FLX925 (AMG-925)

UNC-2025

G-749

CGP52421

AFG210

AAE871

AFG206

Ast-487

XL999

N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide

AUZ454

FI-700

LBW242

TTT-3002

AZD-2932

4SC-203

LY2457546

TG02 (SB1317)

PACRITINIB

SB1578

2-(3,4-Dimethoxy-benzoylamino)-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid amide

3-PHENYL-1H-BENZOFURO[3,2-C]PYRAZOLE

LESTAURTINIB

Tandutinib

AZD1152-HQPA

Linifanib

目录项下的产品

1000669-72-6 / MFCD100669726
KW-2449 is a novel multikinase inhibitor, which suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Recent research showed that HDACIs increase KW-2449 lethality in Bcr/Abl(+) cells in association with inhibition of Bcr/Abl, generation of ROS, and induction of DNA damage. This strategy preferentially targets primary Bcr/Abl(+) hematopoietic cells and exhibits enhanced in vivo activity. Combining KW-2449 with HDACIs warrants attention in IM-resistant Bcr/Abl(+) leukemias. (source: Clin Cancer Res. 2011 May 15;17(10):3219-32. Epub 2011 Apr 7.).
NameC

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1025065-69-3 / MFCD125065693
SGI-1776
N-[(1-甲基-4-哌啶基)甲基]-3-[3-(三氟甲氧基)苯基]-咪唑并[1,2-b]哒嗪-6-胺

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中华人民共和国

1032265-67-0 / MFCD132265670
SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Moreover, SIM010603 inhibited endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.

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1055412-47-9 / MFCD155412479
SU5614
(Z)-5-氯-3-((3,5-二甲基-1H-吡咯-2-基)亚甲基)吲哚啉-2-酮

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1146944-35-5 / MFCD246944355
KRC-108

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1175017-90-9 / MFCD275017909
AKN-028

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1327167-19-0 / MFCD427167190
BPR1J-097

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1395051-72-5 / MFCD495051725
BPR1J-340

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1401033-86-0 / MFCD501033860
FLX925 (AMG-925)

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1429881-91-3 / MFCD529881913
UNC-2025
反式-4-(2-(丁胺基)-5-(4-((4-甲基哌嗪-1-基)甲基)苯基)-7H-吡咯并[2,3-d]嘧啶-7-基)环己醇

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1457983-28-6 / MFCD557983286
8-Bromo-2-((1-Methylpiperidin-4-Yl)Amino)-4-((4-Phenoxyphenyl)Amino)Pyrido[4,3-D]Pyrimidin-5(6H)-One
8-溴-2-((1-甲基哌啶-4-基)氨基)-4-((4-苯氧基苯基)氨基)吡啶并[4,3-d]嘧啶-5(6H)-酮

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179237-49-1 / MFCD79237491
CGP52421

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228400-22-4 / MFCD28400224
AFG210

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289479-07-8 / MFCD89479078
AAE871 is a type I FLT3 inhibitor.

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630122-37-1 / MFCD30122371
AFG206

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630124-46-8 / MFCD30124468
AST487, also known as NVP-AST487, is a RET kinase inhibitor/FLT3 inhibitor. The RET kinase has emerged as a promising target for the therapy of medullary thyroid cancers (MTC) and of a subset of papillary thyroid cancers. NVP- AST487 has an IC(50) of 0.88 mumol/L on RET kinase, inhibits RET autophosphorylation and activation of downstream effectors, and potently inhibited the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. NVP- AST487 induced a dose-dependent growth inhibition of xenografts of NIH3T3 cells expressing oncogenic RET, and of the MTC cell line TT in nude mice. NVP- AST487 inhibited calcitonin gene expression in vitro in TT cells, in part, through decreased gene transcription.
1-(4-((4-乙基哌嗪-1-基)甲基)-3-(三氟甲基)苯基)-3-(4-((6-(甲基氨基)嘧啶-4-基)氧基)苯基)脲

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705946-27-6 / MFCD05946276
XL999, a Spectrum Selective Kinase Inhibitor(TM) (SSKIs), is a potent inhibitor of key RTKs implicated in the development and maintenance of tumor vasculature and in the proliferation of some tumor cells. It inhibits the FGFR, VEGFR and PDGFR RTKs and exhibited excellent activity in target-specific cellular functional assays. In addition, XL999 is a potent inhibitor of FLT3, an important driver of leukemia cell proliferation in some patients with acute myelogenous leukemia (AML). In several preclinical models of human tumors, including breast, lung, colon and prostate cancer, XL999 demonstrated potent inhibition of tumor growth, and also caused regression of large well-established tumors.

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850879-09-3 / MFCD50879093
N-(Benzo[D][1,3]Dioxol-5-Ylmethyl)-4-(Benzofuro[3,2-d]Pyrimidin-4-Yl)Piperazine-1-Carbothioamide
N-(苯并[d][1,3]二氧杂环戊烷-5-基甲基)-4-(苯并呋喃并[3,2-d]嘧啶-4-基)哌嗪-1-甲硫酰胺

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853299-07-7 / MFCD53299077
1-(4-((2-Aminopyrimidin-4-Yl)Oxy)Phenyl)-3-(4-((4-Methylpiperazin-1-Yl)Methyl)-3-(Trifluoromethyl)Phenyl)Urea
1-(4-(2-氨基嘧啶-4-基氧基)苯基)-3-(4-((4-甲基哌嗪-1-基)甲基)-3-三氟甲基苯基)脲

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866883-79-6 / MFCD66883796
FI-700

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867324-12-7 / MFCD67324127
LBW242

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871037-95-5 / MFCD71037955
TTT-3002

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883986-34-3 / MFCD83986343
AZD-2932 is a high affinity inhibitor of VEFGR-2 and PDGFR. AZD-2932 has a balanced ~ 1:1 ratio of activity vs both VEGFR-2 and PDGFRβ and shows IC50 values of 8 and 4 nM against the two enzymes, respectively. It is also active on c-Kit and FLT3 with good selectivity on a panel of kinases. The pharmacokinetic behavior and the preclinical antitumor activity in nude mice bearing C6 rat glial tumors indicate that 31 has the potential to become an antiangiogenic agent in the clinic.

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895533-09-2 / MFCD95533092
4SC-203

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908265-94-1 / MFCD008265941
LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 syngeneic rat mammary tumor models. Additionally, LY2457546 caused complete regression of well-established tumors in an acute myelogenous leukemia (AML) FLT3-ITD mutant xenograft tumor model. The unique spectrum of target activity, potent in vivo anti-tumor efficacy in a variety of rodent and human solid tumor models, exquisite potency against a clinically relevant model of AML, and non-clinical safety profile justify the advancement of LY2457546 into clinical testing. (source: Invest New Drugs. 2012

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937270-47-8 / MFCD037270478
TG02, also known as SB1317, is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. It dose-dependently inhibits signaling pathways downstream of CDKs, JAK2 and FLT3 in cancer cells with the main targets being CDKs. TG02 is anti-proliferative in a broad range of tumor cell lines, inducing G1 cell cycle arrest and apoptosis. In vivo, TG02 exhibits favorable pharmacokinetics after oral dosing in xenograft models and accumulates in tumor tissues, inducing an effective blockade of both CDK and STAT signaling.

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937272-79-2 / MFCD037272792
PACRITINIB
Pacritinib游离态

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937273-04-6 / MFCD037273046
SB1578

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301305-73-7 / MFCD00617269
2-(3,4-Dimethoxybenzamido)-4,5,6,7-Tetrahydrobenzo[B]Thiophene-3-Carboxamide
2-(3,4-二甲氧基苯甲酰胺基)-4,5,6,7-四氢苯并[b]噻吩-3-甲酰胺

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中华人民共和国
√

34823-86-4 / MFCD01416326
3-Phenyl-1H-Benzofuro[3,2-c]Pyrazole
3-苯基-1H-苯并呋喃并[3,2-c]吡唑

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111358-88-4 / MFCD09837744
LESTAURTINIB

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387867-13-2 / MFCD09954147
N-(4-Isopropoxyphenyl)-4-(6-Methoxy-7-(3-(Piperidin-1-Yl)Propoxy)Quinazolin-4-Yl)Piperazine-1-Carboxamide
N-(4-异丙氧基苯基)-4-(6-甲氧基-7-(3-(哌啶-1-基)丙氧基)喹唑啉-4-基)哌嗪-1-甲酰胺

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722544-51-6 / MFCD10687152
3-[[7-[3-[Ethyl(2-Hydroxyethyl)Amino]Propoxy]-4-Quinazoline]Amino]-N-(3-Fluorophenyl)-1H-Pyrazole-3-Acetamide
5-[[7-[3-[乙基(2-羟基乙基)氨基]丙氧基]-4-喹唑啉]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺

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中华人民共和国
√

796967-16-3 / MFCD11840918
1-(4-(3-Amino-1H-Indazol-4-Yl)Phenyl)-3-(2-Fluoro-5-Methylphenyl)Urea
1-(4-(3-氨基-1H-吲唑-4-基)苯基)-3-(2-氟-5-甲基苯基)脲

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中华人民共和国
√

FLT3

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FLT3

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