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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
18 Results for "
FLT3-ITD mutation
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "FLT3-ITD mutation" in MCE Product Catalog:
48
48 Cited Publications
Synonyms: AC220 dihydrochloride
Quizartinib (AC220) dihydrochloride is an orally active, potent and selective FLT3 inhibitor. Quizartinib dihydrochloride inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib dihydrochloride inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib dihydrochloride can be used for the research of cancer .
Cat. No.: HY-172581
CAS No.: 1862226-99-0
Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia .
Cat. No.: HY-162037
CAS No.: 2241659-94-7
CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation .
Cat. No.: HY-115443
CAS No.: 2089590-80-5
MZH29 is a potent and orally active FLT3 inhibitor. MZH29 shows inhibitory effects on wild-type and mutant FLT3, including the FLT3-ITD, FLT3-D835H/Y/V and FLT3-K663Q mutants. MZH29 retains its potent inhibitory effect against the FLT3-ITD/F691L mutation, a drug resistance mutation against the well-known FLT3 inhibitor, AC220 (HY-13001). MZH29 can be used for the research of cancer, such as acute myeloid leukemia (AML) .
Cat. No.: HY-145691
CAS No.: 381173-58-6
HP1142 is a potent and selective inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1142 is a benzoimidazole scaffold-based compound. HP1142 has the potential for the research of FLT3/ITD leukemia .
Cat. No.: HY-145690
CAS No.: 2245074-20-6
HP1328 is a potent inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1328 is a benzoimidazole scaffold-based compound. HP1328 significantly reduces the leukemia burden and prolongs the survival of mice with FLT3/ITD leukemia .
Cat. No.: HY-13001R
CAS No.: 950769-58-1
Synonyms: AC220 (Standard)
Quizartinib (AC220) (Standard) is the analytical standard of Quizartinib (HY-13001). This product is intended for research and analytical applications. Quizartinib is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer .
Cat. No.: HY-170576
FLT3-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 .
Cat. No.: HY-155770
FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor with IC50 values of 1 and 4 nM for FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-20 has anti-proliferation efficacy in FLT3-ITD-positive AML cell lines MV4-11 and MOLM-13 (7 and 9 nM, respectively) and the MOLM-13 variant (4 nM) with the FLT3-ITD-D835Y mutation. FLT3-IN-20 can be used in research of cancer .
Cat. No.: HY-E70724
FLT3 (FMS-like tyrosine kinase 3, CD135) is a type 3 receptor tyrosine kinase that plays important roles in cell survival, proliferation, and differentiation during normal hematopoiesis. FLT3 is one of the most frequently mutated genes in acute myeloid leukemia (AML). FLT3 ITD is a internal tandem duplication (ITD) mutation of FLT3 that may be present in AML cells. FLT3 ITD Recombinant Human Active Protein Kinase is a recombinant FLT3 ITD protein that can be used to study FLT3 ITD-related functions .
Cat. No.: HY-155594
CAS No.: 2143089-35-2
LT-540-717 (compound 32) is a potent FLT3 inhibitor (IC50=0.62 nM) with antiproliferative activity. LT-540-717 also inhibits several acquired FLT3 mutations, FLT3 (ITD, D835V), FLT3 (ITD, F691L), FLT3 (D835Y) and FLT3 (D835V). LT-540-717 has potential to be an anti-AML agent .
Cat. No.: HY-156410
CAS No.: 2489528-97-2
FLT3-IN-23 (compound 15) is an inhibitor of JFMS-like tyrosine kinase 3 (FLT3) with an IC50 of 7.42 nM. FLT3-IN-23 has antiproliferative activities against BaF3 cells carrying various FLT3-TKD and FLT3-ITD-TKD mutations .
Cat. No.: HY-155112
CAS No.: 2713553-88-7
Target:
Research Areas:
Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .
Cat. No.: HY-122670
CAS No.: 1627962-21-3
VS-II-173 is a pan-Pim kinase inhibitor with IC50 values of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPKα1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .
Cat. No.: HY-175900
CAS No.: 3031481-63-4
Research Areas:
FLT3 ligand-4 (Intermediate of compound 35) is a FLT3 ligand that can be used to synthesize PROTAC degrader (HY-161280) targeting FLT3 degradation. FLT3 ligand-4 is applicable to research related to acute myeloid leukemia .
Cat. No.: HY-179734
Research Areas:
PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC50 of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
