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PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC50s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1 wt, KIT wt, PDGFRR wt .
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
PDGFRα kinase-IN-2 is a potent PDGFR-α inhibitor with an IC50 of 2.1 nM. PDGFRα kinase-IN-2 exhibits anticancer activity against human colon cancer HT-29 cell with an IC50 of 1.48 μM. PDGFRα kinase-IN-2 has anti-angiogenic activity in zebrafish models and low embryonic lethality. PDGFRα kinase-IN-2 can used for the studies of colon cancer and anti-angiogenesis .
PDGFRα kinase inhibitor 3 (Compound L7) is a highly potent inhibitor targeting the PDGFRαD842V kinase with IC50s values of 23.8 nM and 2.1 nM in biochemical and cellular assays, respectively. PDGFRα kinase inhibitor 3 binds to the ATP-binding pocket of PDGFRαD842V to block its downstream signaling pathways and inhibit kinase activity. PDGFRα kinase inhibitor 3 can be used for gastrointestinal stromal tumors (GISTs) study .
PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of 0.153 and 0.004 μM, respectively. PDGFRα/FLT3-ITD-IN-3 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
PDGFRα/FLT3-ITD-IN-1 (Compound 12d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
PDGFRα/FLT3-ITD-IN-2 (Compound 13d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 20 and 1.654 μM, respectively. PDGFRα/FLT3-ITD-IN-2 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
Necroptosis-IN-4, a potent necroptosis inhibitor, is a RIP kinase 1 (RIPK1) inhibitor. Necroptosis-IN-4 has no inhibitory activity against RIPK3 and weak inhibitory activity against VEGFR1/2 and PDGFR-α .
Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model .
Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody that selectively blocks the PDGFRα signal transduction. Tovetumab can be used in the research of glioblastoma and non-small cell lung cancer (NSCLC) .
Olaratumab (IMC-3G3; LY3012207) is an anti-platelet-derived growth factor receptor alpha (PDGFRα) human monoclonal IgG1 antibody with antitumor activity .
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .
Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC50 values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer .
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension .
Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .
Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
Cediranib (maleate) (Standard) is the analytical standard of Cediranib (maleate). This product is intended for research and analytical applications. Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma .
Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .
Cediranib (Standard) is the analytical standard of Cediranib. This product is intended for research and analytical applications. Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
Multi-kinase inhibitor 4 (compound 14) is an orally active inhibitor of FLT1, KDR, FLT3, FLT4, PDGFRα, PDGFRβ, with IC50s of 1.97 nM, 1.04 nM, 0.33 nM, 1.44 nM, 0.18 nM, 0.89 nM. Multi-kinase inhibitor 4 plays an important role in cancer research .
ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
Ponatinib (hydrochloride) (Standard) is the analytical standard of Ponatinib (hydrochloride). This product is intended for research and analytical applications. Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .
Sutetinib is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo .
GW694590A (UNC10112731) is a MYC protein stabilizer that increases endogenous MYC protein levels. GW694590A also targets receptor tyrosine kinases, inhibiting DDR2, KIT and PDGFRα by 81% at 1 μM. , 68% and 67%. GW694590A is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential effects on the Fluc reporter gene .
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
SU9518 is a tyrosine kinase inhibitor with specific activity against PDGFRα. SU9518 can inhibit the development of proliferative vitreoretinopathy (PVR) in fibroblast and Muller cell rabbit models. SU9518 showed effective inhibitory effects in these models without toxic effects. Therefore, SU9518 has the potential to be used to inhibit PVR in humans and other proliferative eye diseases involving fibrosis and gliosis .
Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo .
Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects .
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively .
MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells .
Amuvatinib (Standard) is the analytical standard of Amuvatinib. This product is intended for research and analytical applications. Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension .
Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition .
Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody that selectively blocks the PDGFRα signal transduction. Tovetumab can be used in the research of glioblastoma and non-small cell lung cancer (NSCLC) .
Olaratumab (IMC-3G3; LY3012207) is an anti-platelet-derived growth factor receptor alpha (PDGFRα) human monoclonal IgG1 antibody with antitumor activity .
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively .
PDGF R alpha protein is a tyrosine protein kinase receptor for PDGFA, PDGFB, and PDGFC that coordinates embryonic development, cell proliferation, survival, and chemotaxis. Their functions vary, promoting or inhibiting cell proliferation and migration depending on the situation. PDGF R alpha Protein, Rat (HEK293, His) is the recombinant rat-derived PDGF R alpha protein, expressed by HEK293 , with C-His labeled tag.
PDGF R α is a tyrosine protein kinase and an important cell surface receptor for PDGFA, PDGFB and PDGFC, affecting embryonic development, cell proliferation, survival and chemotaxis. Its effects on cell behavior vary, promoting or inhibiting proliferation and migration depending on environmental cues. PDGF R alpha Protein, Human (HEK293, Fc) is the recombinant human-derived PDGF R alpha protein, expressed by HEK293 , with C-hFc labeled tag.
PDGF R alpha protein is a tyrosine protein kinase receptor for PDGFA, PDGFB, and PDGFC that coordinates embryonic development, cell proliferation, survival, and chemotaxis. Their functions vary, promoting or inhibiting cell proliferation and migration depending on the situation. PDGF R alpha Protein, Rat (HEK293, Fc) is the recombinant rat-derived PDGF R alpha protein, expressed by HEK293 , with C-hFc labeled tag.
PDGF R α is a tyrosine-protein kinase receptor with critical effects on embryonic development, cell proliferation, survival, and chemotaxis. Its effects on cell behavior vary depending on the environment and is critical for differentiation of bone marrow mesenchymal stem cells, normal skeletal development, embryonic skull closure, and gastrointestinal mucosal formation. PDGF R alpha Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived PDGF R alpha protein, expressed by HEK293 , with C-hFc labeled tag.
Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
PDGFR alpha Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 123 kDa, targeting to PDGFR alpha. It can be used for WB,ICC,IHC-P,FC assays with tag free, in the background of Human, Mouse.
