FLT3 Inhibitor
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PROTAC FLT-3 degrader 4
0 ImagesCat. No.: HY-158325CAS No.: 2956722-48-6PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor).
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HI042
0 ImagesCat. No.: HY-175473CAS No.: 898168-15-5HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication (FLT3-|TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML).
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SU11657
0 ImagesCat. No.: HY-138032CAS No.: 326914-17-4Synonyms: N,N-Dimethyl sunitinibSU11657 (N,N-Dimethyl sunitinib) is an orally active multi-targeted tyrosine kinase inhibitor with IC50 values of 0.04 μM (c-Kit), 0.005 μM (PDGFR), 0.013 μM (VEGFR1), 0.017 μM (VEGFR2) and 50 nM (FLT3), respectively. SU11657 exhibits anti-angiogenic activity. SU11657 delays leukemia progression, synergizes with ATRA (HY-14649) to reduce leukemia burden, and inhibits symptoms and tissue damage associated with rheumatoid arthritis. SU11657 can be used in research related to FLT3-mutated acute promyelocytic leukemia, rheumatoid arthritis, neuroblastoma, and benign/atypical meningioma.
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CG-3-246
0 ImagesCat. No.: HY-170689CAS No.: 3107307-79-6CG-3-246 is a dual inhibitor of FLT3/BCL-2, with the Kds of 63 and 4.25 nM, respectibely. CG-3-246 plays an important role in acute myeloid leukemias research.
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L-783277
0 ImagesCat. No.: HY-123586CAS No.: 791807-02-8L-783277 (Compound 4) is a MEK inhibitor (IC50 = 4 nM). L-783277 has potent inhibitory activity against a variety of kinases, including VEGFR2/3, FLT1/3/4, MEK1/2, KDR, and PDGFRα, but has low selectivity for the kinase community. L-783277 inhibits viability (IC50 = 22 mM) and cell proliferation (IC50 = 21 mM) of H295R cells. L-783277 could be used in research on cancers such as adrenocortical carcinoma.
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FGFRs-IN-1
0 ImagesCat. No.: HY-170846FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model.
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FYJ-195
0 ImagesCat. No.: HY-184161FYJ-195 is a potent orally active FLT3 inhibitor targeting FLT3 and its variants FLT3-ITD, FLT3-F691L, FLT3-D835V, FLT3-D835Y. FYJ-195 blocks FLT3 autophosphorylation and downstream STAT5, AKT, ERK signaling pathways, and induces apoptosis. FYJ-195 induces tumor regression in mouse acute myeloid leukemia (AML) xenograft models. FYJ-195 can be used for the research of AML.
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FLT3-IN-28
0 ImagesCat. No.: HY-170576FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD.
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Sorafenib-d3 tosylate
0 ImagesCat. No.: HY-10201S4CAS No.: 1333386-17-6Synonyms: Donafenib tosylate; Bay 43-9006-d3 tosylateSorafenib-d3 (Donafenib) tosylate is the deuterated-labeled Sorafenib tosylate (HY-10201A). Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
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PLM-101
0 ImagesCat. No.: HY-149539PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po).
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Zotiraciclib hydrochloride
0 ImagesCat. No.: HY-15163ACAS No.: 1354567-82-0Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies.
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FLT3-IN-32
0 ImagesCat. No.: HY-174437CAS No.: 3047195-48-9FLT3-IN-32 is a potent and orally active FLT3 inhibitor. FLT3-IN-32 shows high selectivity for FLT3 and efficiently inhibits FLT3-activating mutations and induces apoptosis. FLT3-IN-32 shows good tolerability in non-tumor bearing mice. FLT3-IN-32 demonstrates outstanding anti-tumor efficacy in MV4-11 bearing NOD/SCID mice, prolonging the survival noticeably. FLT3-IN-32 can be used for the research of acute myeloid leukemia.
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FLT3-IN-34
0 ImagesCat. No.: HY-178020CAS No.: 3020729-11-4FLT3-IN-34 is a FLT3 inhibitor, with an IC50 value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML).
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LT-850-166
0 ImagesCat. No.: HY-139619CAS No.: 3031480-22-2
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HSB401
0 ImagesCat. No.: HY-179382CAS No.: 3022265-51-3HSB401 is an orally active FLT3 inhibitor (IC50: 28, 5, 72, 51 nM for FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, FLT3-ITD, respectively). HSB401 downregulates FLT3 signaling and induces cell cycle arrest and apoptosis. HSB401 spares c-KIT inhibition, thereby reducing the risk of myelosuppression. HSB401 significantly suppresses tumor growth in the MV4-11 xenograft mouse model. HSB401 can be used for the research of acute myeloid leukemia.
