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FLT3/D835Y

" in MedChemExpress (MCE) Product Catalog:

By Targets:	FLT3 (42) Akt (1) Apoptosis (13) Aurora Kinase (1) Bcr-Abl (1) c-Kit (1) Checkpoint Kinase (Chk) (2) Cytochrome P450 (1) FAK (1) FGFR (4) IRAK (1) Isotope-Labeled Compounds (1) JAK (6) p38 MAPK (1) Reactive Oxygen Species (ROS) (2) Reference Standards (1) STAT (1)
By Research Areas:	Cancer (42) Inflammation/Immunology (4)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: FLT3

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-16379

Pacritinib Maximum Cited Publications 19 Publications Verification SB1518	JAK FLT3	Cancer
Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2 ^V617F mutant (IC₅₀=19 nM). Pacritinib also inhibits *FLT3* (IC₅₀=22 nM) and its mutant FLT3 ^D835Y (IC₅₀=6 nM).

HY-145015

Tuspetinib HM43239	FLT3 Apoptosis	Cancer
Tuspetinib (HM43239) is an orally active and selective *FLT3* inhibitor with IC₅₀s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells ^[3].

HY-12333

Denfivontinib 2 Publications Verification G-749	FLT3 Apoptosis	Cancer
Denfivontinib (G-749) is a potent, oral active and ATP competitive *FLT3* inhibitor, with IC₅₀s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML) .

HY-153857

Lasmotinib PHI-101	FLT3 Checkpoint Kinase (Chk)	Cancer
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 ^[3] .

HY-18161

CCT241736	FLT3 Aurora Kinase	Cancer
CCT241736 is a potent and orally bioavailable dual *FLT3* and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A K_d, 7.5 nM, IC₅₀, 38 nM; Aurora-B K_d, 48 nM), FLT3 kinase (K_d, 6.2 nM), and FLT3 mutants including FLT3-ITD (K_d, 38 nM) and FLT3(D835Y) (K_d, 14 nM).

HY-145723

MAX-40279 1 Publications Verification	FLT3 FGFR	Inflammation/Immunology Cancer
MAX-40279 is a dual and orally active inhibitor of *FLT3* kinase and FGFR kinase. MAX-40279 is also effective against the FLT3 mutants such as FLT3 ^D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 can be used for the research of acute myelogenous leukemia (AML) ^[3].

HY-112145

FLT3-IN-3 3 Publications Verification	FLT3	Cancer
FLT3-IN-3 is a potent *FLT3* inhibitor with IC₅₀s of 13 and 8 nM for FLT3 WT and **FLT3 D835Y**, respectively.

HY-148070

FLT3-IN-17	FLT3 FAK Cytochrome P450	Cancer
FLT3-IN-17 inhibits CYPs and *FLT3* mutants activity (IC₅₀s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC₅₀ value of 12 nM. FLT3 ligand-2 can be used in the research of cancers .

HY-E70723

FLT3 D835Y Recombinant Human Active Protein Kinase	FLT3	Cancer
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 .

HY-16379B

Pacritinib citrate Maximum Cited Publications 19 Publications Verification SB1518 citrate	JAK FLT3	Cancer
Pacritinib (SB1518) citrate is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2 ^V617F mutant (IC₅₀=19 nM). Pacritinib citrate also inhibits *FLT3* (IC₅₀=22 nM) and its mutant FLT3 ^D835Y (IC₅₀=6 nM). Pacritinib citrate can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) ^[3].

HY-18949

JI6	FLT3 JAK c-Kit	Cancer
JI6 is a potent, selective and orally active *FLT3* inhibitor, with IC₅₀s of ～40, 8, and 4 nM for *FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3* and c-Kit, with IC₅₀s of ～250 and ～500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia .

HY-16379S

Pacritinib-d4 SB1518-d₄	Isotope-Labeled Compounds JAK FLT3	Cancer
Pacritinib-d₈ (SB1518-d₈) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2 ^V617F mutant (IC₅₀=19 nM). Pacritinib also inhibits *FLT3* (IC₅₀=22 nM) and its mutant FLT3 ^D835Y (IC₅₀=6 nM).

HY-143434

FLT3/D835Y-IN-1	FLT3	Cancer
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective *FLT3* and *FLT3/D835Y* inhibitor, with IC₅₀ values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia) .

HY-161323

FLT3-ITD/D835Y-IN-1	FLT3 Bcr-Abl Apoptosis	Cancer
FLT3-ITD/D835Y-IN-1 (Compound 1) is a *FLT3-ITD* and BCR-ABL inhibitor. FLT3-ITD/D835Y-IN-1 mediates proapoptosis by inhibiting the FLT3 and BCR-ABL pathways, as well as other possible targets. FLT3-ITD/D835Y-IN-1 can be used in the study of acute myeloid leukemia (AML) .

HY-125008

JH-IX-179	FLT3 Apoptosis	Cancer
JH-IX-179 is an *FLT3* inhibitor (IC₅₀ = 4 nM (FLT3-ITD), 10 nM (FLT3-D835Y)). JH-IX-179 inhibits G1 phase arrest and induces apoptosis in FLT3-ITD-expressing cells. JH-IX-179 can be used in acute myeloid leukemia (AML) research .

HY-158265

FLT3D835Y/F691L-IN-1	FLT3	Cancer
FLT3D835Y/F691L-IN-1 (compd 8v) is an orally active inhibitor of FLT3 3-tyrosine kinase domain D835Y/F691L secondary mutations with IC₅₀s of 1.5 and 9.7 nM. FLT3D835Y/F691L-IN-1 can be used for acute myeloid leukemia research .

HY-179382

HSB401	FLT3 Apoptosis	Cancer
HSB401 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 .

HY-176735

FLT3/IRAK4-IN-1	IRAK FLT3 Apoptosis	Cancer
FLT3/IRAK4-IN-1 is a selective *FLT3/IRAK4* inhibitor with the remarkable activity towards *FLT3-WT* (IC₅₀ = 1.95 nM), *FLT3-D835Y* (IC₅₀ = 3.22 nM) and IRAK4 (IC₅₀ = 53.72 nM). LT3/IRAK4-IN-1 has relatively low toxicity to normal bone marrow cells, can effectively promote cell apoptosis, and has the potential to overcome drug resistance. FLT3/IRAK4-IN-1 can be used for research on acute myeloid leukemia (AML) .

HY-145015A

Tuspetinib hydrate HM43239 hydrate	FLT3 Apoptosis	Cancer
Tuspetinib (HM43239) hydrate is an orally active and selective *FLT3* inhibitor with IC₅₀s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells ^[3].

HY-145015B

Tuspetinib dihydrochloride HM43239 dihydrochloride	FLT3 Apoptosis	Cancer
Tuspetinib (HM43239) dihydrochloride is an orally active and selective *FLT3* inhibitor with IC₅₀s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib dihydrochloride inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib dihydrochloride inhibits the proliferation and induces the apoptosis of leukemic cells ^[3].

HY-16379A

Pacritinib hydrochloride SB1518 hydrochloride	JAK FLT3	Cancer
Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2 ^V617F mutant (IC₅₀=19 nM). Pacritinib hydrochloride also inhibits *FLT3* (IC₅₀=22 nM) and its mutant FLT3 ^D835Y (IC₅₀=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) ^[3].

HY-145723C

MAX-40279 hemiadipate 1 Publications Verification	FLT3 FGFR	Inflammation/Immunology Cancer
MAX-40279 hemiadipate is a dual and orally active inhibitor of *FLT3* kinase and FGFR kinase. MAX-40279 hemiadipate is also effective against the FLT3 mutants such as FLT3 ^D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 hemiadipate inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemiadipate can be used for the research of acute myelogenous leukemia (AML) ^[3].

HY-155302

FLT3-IN-22	FLT3	Cancer
FLT3-IN-22 (compound 22f) is a potent *FLT3* inhibitor with IC₅₀ values of 0.941 nM and 0.199 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-22 exhibits strong antiproliferative activity against MV4-11 cells and the mutant FLT kinase expressed Ba/F3 cell lines, including FLT-D835Y and FLT3-F691L .

HY-146886

FLT3-IN-15	FLT3	Cancer
FLT3-IN-15 is a highly potent and orally active *FLT3* inhibitor with IC₅₀s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia .

HY-155770

FLT3-IN-20	FLT3	Cancer
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 .

HY-162032

FLT3-IN-25	FLT3	Cancer
FLT3-IN-25 (compound 17) is a potent inhibitor of *FLT3, with IC₅₀s of 1.2 nM, 1.4 nM and 1.1 nM for FLT3-WT, FLT3-D835Y* and FLT3-ITD, respectively. FLT3-IN-25 plays an important role in acute myeloid leukemia (AML) .

HY-174437A

FLT3-IN-32 TFA	FLT3	Cancer
FLT3-IN-32 TFA is a potent *FLT3* inhibitor with an IC₅₀s of 2.40 nM and 3.83 nM against FLT3-ITD and FLT3-D835Y. FLT3-IN-32 TFA inhibits proliferation/survival of human MV4-11 cells with an IC₅₀ of 0.07 nM. FLT3-IN-32 TFA can be used for the study of acute myeloid leukemia (AML) .

HY-143895

FLT3-IN-12	FLT3	Cancer
FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC₅₀s of 1.48 nM and 2.87 nM for *FLT3-WT* and *FLT3-D835Y, respectively. FLT3-IN-12* possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC₅₀ of 0.75 nM) .

HY-174137

FLT3-IN-31	Apoptosis FLT3	Cancer
FLT3-IN-31 (compound 10q) is a potent *FLT3* inhibitor with IC₅₀ values of 0.16, 2.4 nM for FLT3, FLT3-D835Y, resprctively. FLT3-IN-31 shows antiproliferation activity. FLT3-IN-31 decreases the protein expression of p-FLT3, P-STAT5, P-ERK. FLT3-IN-31 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-31 shows antitumor activity .

HY-143894

FLT3-IN-11	FLT3	Cancer
FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC₅₀s of 7.22 nM and 4.95 nM for wild-type FLT3 and *FLT3-D835Y, respectively. FLT3-IN-11* high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC₅₀ of 3.2 nM) .

HY-170640

FLT3-IN-29	FLT3 Reactive Oxygen Species (ROS) Apoptosis	Cancer
FLT3-IN-29 (Compound MY-10) is a *FLT3* inhibitor (IC₅₀s: 6.5 and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants). FLT3-IN-29 arrests cell cycle at the G0/G1 phase and efficiently induces Apoptosis. FLT3-IN-29 also reduces reactive oxygen species (ROS) production and mitochondrial membrane potential (MMP). FLT3-IN-29 displays antileukemic activity .

HY-155594

LT-540-717	FLT3	Cancer
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 .

HY-144711

FLT3/ITD-IN-3	FLT3	Cancer
FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC₅₀ values of 0.3, 0.4 and 0.9 nM against FLT3 ^D835Y, *FLT3* and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .

HY-144710

FLT3/ITD-IN-2	FLT3	Cancer
FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC₅₀ values of 0.3, 0.4 and 1.0 nM against FLT3 ^D835Y, *FLT3* and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .

HY-174437B

FLT3-IN-32 hydrochloride	FLT3 Apoptosis STAT p38 MAPK Akt	Cancer
FLT3-IN-32 hydrochloride is a potent and orally active *FLT3* inhibitor with an IC₅₀s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML) .

HY-162367

FLT3/CHK1-IN-2	FLT3 Checkpoint Kinase (Chk)	Cancer
FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of *FLT3* and CHK1, with IC₅₀s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML) .

HY-126920

AFG206	FLT3 Apoptosis	Cancer
AFG206 is a first-generation ATP competitive “type II” *FLT3* inhibitor. AFG206 potently inhibits cell proliferation (IC₅₀ around 0.1 µM) via induction of Apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells. AFG206 is promising for research of acute myeloid leukemia .

HY-145723A

MAX-40279 hydrochloride	FLT3 FGFR	Inflammation/Immunology Cancer
MAX-40279 hydrochloride is a dual and orally active inhibitor of *FLT3* kinase and FGFR kinase. MAX-40279 hydrochloride is also effective against the FLT3 mutants such as FLT3 ^D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 hydrochloride inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hydrochloride can be used for the research of acute myelogenous leukemia (AML) ^[3].

HY-123201

KRN383 analog	FLT3	Cancer
KRN383 analog is an analog of KRN383. KRN383 is an orally active *Flt3* inhibitor that inhibits the autophosphorylation of Flt3 bearing internal tandem duplications (ITDs) and the Asp835Tyr (D835Y) point mutation with IC₅₀ values of < or =5.9 and 43 nM, respectively. KRN383 also inhibits the proliferation of the ITD-positive cell lines with IC₅₀ values of < or =2.9 nM. KRN383 can be used for the research of acute myeloid leukemia .

HY-145723B

MAX-40279 hemifumarate 1 Publications Verification	FLT3 FGFR	Inflammation/Immunology Cancer
MAX-40279 hemifumarate is a dual and orally active inhibitor of *FLT3* kinase and FGFR kinase. MAX-40279 hemifumarate is also effective against the FLT3 mutants such as FLT3 ^D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 hemifumarate inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemifumarate can be used for the research of acute myelogenous leukemia (AML) ^[3].

HY-181945

FLT3-IN-39	FLT3 Apoptosis Reactive Oxygen Species (ROS)	Cancer
FLT3-IN-39 (Compound W4) is a selective *FLT3* inhibitor, with an IC₅₀ value of 16.0 nM against *FLT3*-ITD and an IC₅₀ value of 20.4 nM against *FLT3*-D835Y. FLT3-IN-39 inhibits *FLT3*-ITD and *FLT3*-D835Y mutant kinases. FLT3-IN-39 induces G0/G1 cell cycle arrest and Apoptosis in cancer cells, and reduces intracellular ROS levels. FLT3-IN-39 exhibits anti-tumor activity against acute myeloid leukemia .

HY-16379R

Pacritinib (Standard) SB1518 (Standard)	Reference Standards JAK FLT3	Cancer
Pacritinib (Standard) is the analytical standard of Pacritinib. This product is intended for research and analytical applications. Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).

Pacritinib-d4
Pacritinib-d₈ (SB1518-d₈) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2 ^V617F mutant (IC₅₀=19 nM). Pacritinib also inhibits *FLT3* (IC₅₀=22 nM) and its mutant FLT3 ^D835Y (IC₅₀=6 nM).

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