目录号 | 产品详情 | 靶点 | |
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T68389 | |||
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 D...... | |||
T11638 | Aurora Kinase | ||
Ilorasertib hydrochloride (ABT-348 hydrochloride) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A (IC50s: 1 nM, 7 nM, 120 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM). | |||
T71382 | |||
KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumor growth in human HT29 colorectal cancer and NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice. This molecule should serve as a useful lead for inhibitors targeting kinases and may lead to new therapeutics for the treatment of cancer. (source: Invest New Drugs. 2012 Apr;30(2):518-23. doi: 10.1007/s10637-010-9584-2. Epub 2010 Nov 16. ). | |||
T62417 | |||
MELK-8a (NVS-MELK8a) 是一种高效的、选择性的母体胚胎亮氨酸拉链激酶 (MELK) 抑制剂 (IC50: 2 nM)。MELK-8a 也能够抑制 Flt3 (ITD) (IC50: 0.18 μM)、Haspin (IC50: 0.19 μM)、PDGFRα (IC50: 0.42 μM)。其中 MELK 在调节癌细胞的细胞有丝分裂中具有重要作用。 | |||
T64283 | |||
Pacritinib hydrochloride 是一种野生型 JAK2 (IC50: 23 nM) 和 JAK2V617F 突变型 (IC50: 19 nM) 的有效抑制剂。Pacritinib hydrochloride 也能够抑制 FLT3 (IC50: 22 nM) 及其突变型 FLT3D835Y (IC50: 6 nM)。Pacritinib hydrochloride 能够用于研究急性髓系白血病(AML)和骨髓纤维化(MF)。 | |||
T9470 | MAPK | ||
HPK1-IN-7 是一种口服有活性的、有效的HPK1(造血祖细胞激酶1, MAP4K1) 抑制剂,其IC50值为2.6 nM,具有强大的家族及激酶组选择性。它对 IRAK4 (59 nM) 和 GLK (140 nM) 具有选择性。当它与抗 PD1联合使用时,对 MC38 同基因肿瘤模型表现出极大的疗效。 | |||
T13564L | EGFR IGF-1R | ||
AZ7550 hydrochloride (AZ7550 hydrochloride ) 是 AZD9291 的活性代谢物,可抑制 IGF1R 活性,IC50为 1.6 μM。 | |||
T13564 | MLK FAK EGFR FLT Tyrosine Kinases PYK2 MNK IGF-1R ACK BTK ALK Drug Metabolite | ||
AZ7550 是 AZD9291 的活性代谢物,可抑制 IGF1R 活性,IC50为 1.6 μM。 | |||
T21062 | |||
TAK-659 is a spleen tyrosine kinase (SYK) inhibitor. | |||
T14055 | VEGFR FLT MEK MAPK PDGFR Antibiotic Src | ||
5Z-7-Oxozeaenol (FR148083) 是一种天然抗原生动物抑制剂,不可逆的选择性抑制 TAK1和 VEGF-R2,IC50值分别为 8 nM 和 52 nM。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPK-00929 | FLT3 Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
Flt‑3 Ligand, also known as FL, is an alpha -helical cytokine that promotes the differentiation of multiple hematopoietic cell lineages.Stimulates the proliferation of early hematopoietic cells by activating FLT3. Synergizes well with a number of other colony stimulating factors and interleukins. FLT3 Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 84.78 kDa and the accession number is Q00342.
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TMPK-00125 | FLT3 Ligand Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Flt‑3 Ligand, also known as FL, is an alpha -helical cytokine that promotes the differentiation of multiple hematopoietic cell lineages.Stimulates the proliferation of early hematopoietic cells by activating FLT3. Synergizes well with a number of other colony stimulating factors and interleukins. FLT3 Ligand Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 44.8 kDa and the accession number is P49771-1.
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TMPY-06873 | FLT3 Ligand Protein, Human, Recombinant | Human | E. coli | ||
FLT3 Ligand Protein, Human, Recombinant is expressed in E. coli expression system. The predicted molecular weight is 17.75 kDa and the accession number is P49771-1.
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TMPY-03066 | FLT3 Ligand Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
FLT3 Ligand Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 45.4 kDa and the accession number is P49772-1.
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TMPY-03215 | FLT3 Ligand Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
FLT3 Ligand Protein, Human, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 20.2 kDa and the accession number is P49771-1.
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TMPY-01247 | FLT3 Protein, Human, Recombinant (T227M, His) | Human | HEK293 Cells | ||
FLT3 Protein, Human, Recombinant (T227M, His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 59.7 kDa and the accession number is P36888-1.
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TMPK-00523 | FLT3 Protein, Cynomolgus, Recombinant (hFc) | Cynomolgus | HEK293 Cells | ||
FLT3 Protein, Cynomolgus, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 84.58 kDa and the accession number is A0A2K5VQ48.
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TMPK-00416 | FLT3 Protein, Human, Recombinant (His & Avi), Biotinylated | Human | CHO Cells | ||
FLT3 Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in CHO mammalian cells with C-His-Avi tag. The predicted molecular weight is 61.20 kDa and the accession number is P36888-1.
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TMPY-05738 | FLT3 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
FLT3 Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 85.06 kDa and the accession number is P36888-1.
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TMPY-03704 | FLT3 Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
FLT3 Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 69.4 kDa and the accession number is EDL05832.1.
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TMPJ-00123 | FLT3LG Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Fms-related tyrosine kinase 3 ligand(Flt3L) is a single-pass type I membrane protein and consists of 232 amino acids. Flt3L is a hematopoietic four helical bundle cytokine, structurally homologous to stem cell factor and colony stimulating factor. Flt3L synergizes well with a number of other colony stimulating factors and interleukins. Flt3L stimulates the proliferation and differentiation of various blood cell progentiors by activating FLT3.
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TMPY-05332 | FLT3 Ligand Protein, Rat, Recombinant (His) | Rat | Baculovirus Insect Cells | ||
FLT3 Ligand Protein, Rat, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 19.7 kDa and the accession number is NP_001292868.1.
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TMPY-06938 | FLT3 Protein, Human, Recombinant (hFc & Avi), Biotinylated | Human | HEK293 Cells | ||
FLT3 Protein, Human, Recombinant (hFc & Avi), Biotinylated is expressed in HEK293 mammalian cells with hFc and Avi tag. The predicted molecular weight is 86.87 kDa and the accession number is NP_004110.2.
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TMPY-02842 | UBE2L6 Protein, Human, Recombinant (His) | Human | E. coli | ||
UBCH8, also known as UBE2L6, belongs to the ubiquitin-conjugating enzyme family. The family of ubiquitin-conjugating (E2) enzymes is characterized by the presence of a highly conserved ubiquitin-conjugating (UBC) domain. These domains accommodate the ATP-activated ubiquitin (Ub) or ubiquitin-like (UBL) protein via a covalently linked thioester onto its active-site residue. E2 enzymes act via selective protein-protein interactions with the E1 and E3 enzymes and connect activation to covalent modification. By doing so, E2s differentiate effects on downstream substrates, either with a single Ub/UBL molecule or as a chain. UBCH8 is highly similar in primary structure to the enzyme encoded by the UBE2L3 gene. It catalyzes the covalent attachment of ubiquitin or ISG15 to other proteins. UBCH8 functions in the E6/E6-AP-induced ubiquitination of p53/TP53 and promotes ubiquitination and subsequent proteasomal degradation of FLT3. At protein level, it is present in natural killer cells.
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