Scientific Reviews
Product Guides
Blogs
Topics
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
29 Results for "
FLT3 mutations
" in MedChemExpress (MCE) Product Catalog:
Products (29)
29 Results for "FLT3 mutations" in MCE Product Catalog:
4
4 Cited Publications
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
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 .
Synonyms: PHI-101
Target:
Research Areas:
Lasmotinib (PHI-101) is a FLT3 and CHK2 inhibitor. Lasmotinib potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. Lasmotinib synergizes with Venetoclax (HY-15531) or Azacytidine to inhibit leukemia. Lasmotinib exhibits anticancer activity against ovarian and breast cancer .
Cat. No.: HY-170361
CAS No.: 3068001-31-7
Research Areas:
MTHFD2-IN-5 (Compound 16e) is a selective MTHFD2 inhibitor with an IC50 of 66 nM. MTHFD2-IN-5 selectively inhibits MTHFD2. MTHFD2-IN-5 exhibits anticancer activity against acute myeloid leukemia. MTHFD2-IN-5 acts synergistically with Alimta to inhibit the proliferation of acute myeloid leukemia cells .
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-174437
CAS No.: 3047195-48-9
FLT3-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 .
Cat. No.: HY-178061
CAS No.: 2598870-24-5
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
Cat. No.: HY-111249
CAS No.: 871037-95-5
TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research .
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-139619
CAS No.: 3031480-22-2
LT-850-166 is a potent FLT3 inhibitor with the capacity of overcoming a variety of FLT3 mutations.
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-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-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-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-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-E70723
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 D835Y is the most frequent kinase domain mutation, converting aspartic acid to tyrosine. FLT3 D835Y Recombinant Human Active Protein Kinase is a recombinant FLT3 D835Y protein that can be used to study FLT3 D835Y-related functions .
Cat. No.: HY-175473
CAS No.: 898168-15-5
HI042 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) .
- 1
- 2
-
-
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
