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Results for "

AML xenograft mice

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Antibody (1) Akt (2) Apoptosis (9) ATF6 (1) Autophagy (2) Bcl-2 Family (1) c-Myc (2) CDK (2) Ceramidase (1) Checkpoint Kinase (Chk) (1) Dihydroorotate Dehydrogenase (1) DNA/RNA Synthesis (2) Epigenetic Reader Domain (3) ERK (1) FLT3 (4) HIV (1) IKZF Family (1) Influenza Virus (1) JAK (2) Molecular Glues (2) mTOR (1) p38 MAPK (1) p97 (1) PI3K (1) PROTACs (2) Ras (1) STAT (2) Stearoyl-CoA Desaturase (SCD) (1)
By Research Areas:	Cancer (15) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (1)

By Targets:

ADC Antibody (1)

Akt (2)

Apoptosis (9)

ATF6 (1)

Autophagy (2)

Bcl-2 Family (1)

c-Myc (2)

CDK (2)

Ceramidase (1)

Checkpoint Kinase (Chk) (1)

Dihydroorotate Dehydrogenase (1)

DNA/RNA Synthesis (2)

Epigenetic Reader Domain (3)

ERK (1)

FLT3 (4)

HIV (1)

IKZF Family (1)

Influenza Virus (1)

JAK (2)

Molecular Glues (2)

mTOR (1)

p38 MAPK (1)

p97 (1)

PI3K (1)

PROTACs (2)

Ras (1)

STAT (2)

Stearoyl-CoA Desaturase (SCD) (1)

By Research Areas:

Cancer (15)

Inflammation/Immunology (1)

Metabolic Disease (1)

Neurological Disease (1)

Inhibitors & Agonists

Inhibitory Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-155033

SSI-4	Stearoyl-CoA Desaturase (SCD) DNA/RNA Synthesis Apoptosis Autophagy mTOR Influenza Virus	Metabolic Disease Inflammation/Immunology Cancer
SSI-4 is an orally active stearoyl-CoA desaturase (SCD1) inhibitor with an EC₅₀ of 1.9 nM against mouse SCD1. SSI-4 blocks the conversion of saturated fatty acids to monounsaturated fatty acids, reducing the production of oleic acid and palmitoleic acid. SSI-4 induces lipid peroxidation, endoplasmic reticulum stress, DNA damage and activates apoptotic mechanisms. SSI-4 inhibits mTORC1 activity, suppresses B cell proliferation and antibody production, and induces autophagy. SSI-4 is applicable to research on cancers such as acute myeloid leukemia and renal cell carcinoma, as well as influenza infections .

HY-129239

Farudodstat 4 Publications Verification ASLAN003	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Apoptosis	Cancer
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC₅₀ of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice .

HY-15815

Bromosporine 5 Publications Verification	Epigenetic Reader Domain Apoptosis CDK HIV	Cancer
Bromosporine, a chemical probe, is a potent BET inhibitor with an IC₅₀ value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-Fluorouracil (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .

HY-172581

Clifutinib	FLT3 Apoptosis Ras p38 MAPK PI3K Akt JAK STAT	Cancer
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 .

HY-132182

HPA-12 1 Publications Verification	Ceramidase Autophagy Apoptosis ATF6	Neurological Disease Cancer
HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease .

HY-175164

SVC112	Apoptosis c-Myc	Cancer
SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC .

HY-175342

FCN-338 LOXO-338	Bcl-2 Family	Cancer
FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC₅₀ of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL .

HY-175502

MGD-22	Molecular Glues IKZF Family Apoptosis	Cancer
MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC₅₀ values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL) .

HY-178858

PROTAC FLT3/CHK1 Degrader-1	PROTACs FLT3 Checkpoint Kinase (Chk) STAT ERK c-Myc Akt	Cancer
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC₅₀ values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .

HY-174847

VCP/p97 IN-2	p97	Cancer
VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with IC₅₀ of 32 nM for p97. VCP/p97 IN-2 has excellent antitumor activities and significantly inhibits tumor growth in Molm-13 xenograft mice model. VCP/p97 IN-2 can be used for acute myeloid leukemia (AML) research .

HY-175610

PROTAC FLT3/JAK2/BRD4 Degrader-1	PROTACs FLT3 JAK Epigenetic Reader Domain	Cancer
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC₅₀ values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC₅₀ = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .

HY-150562

CDK9-IN-19	CDK	Cancer
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC₅₀ value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .

HY-P991294

MGTA-117 Antibody	ADC Antibody	Cancer
MGTA-117 is a humanized monoclonal antibody targeting CD117. MGTA-117 can be used for synthesis of antibody-drug conjugate (ADC), utilizing an amanitin payload. MGTA-117 has potent anti-tumor activity and increases survival in three acute myeloid leukemia (AML) xenograft hNSG mice models (Kasumi-1, AML PDX 1 and AML PDX 2). MGTA-117 enables hematopoietic stem cell transplantation (HSCT) preprocessing in AML, myelodysplasia with excess blasts (MDS-EB) and gene therapy .

HY-155226

FLT3-IN-21	FLT3 Apoptosis	Cancer
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC₅₀: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC₅₀: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .

HY-124693

DB1055	Apoptosis	Cancer
DB1055 is a HOXA9 inhibitor that competes with HOXA9 binding to DNA (blocking its DNA interaction activity). DB1055 induces in vitro cell growth reduction, cell apoptosis, and differentiation in human acute myeloid leukemia (AML) cells. DB1055 leads to monocyte-to-macrophage differentiation and exhibits antileukemic activities in a human THP-1 AML in vivo model. DB1055 does not impact human CD34⁺ bone marrow cells. DB1055 can be used for the research of acute myeloid leukemia^[1].

HY-181976

dHTC3	Molecular Glues Epigenetic Reader Domain	Others
dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 specifically recruits the first bromodomain of BRD4 to the E3 ubiquitin ligase complex (SCF ^FBXO3), thereby triggering the ubiquitination and degradation of BRD4 .

Cat. No.	Product Name	Target	Research Area	Image

HY-P991294

MGTA-117 Antibody	ADC Antibody	Cancer
MGTA-117 is a humanized monoclonal antibody targeting CD117. MGTA-117 can be used for synthesis of antibody-drug conjugate (ADC), utilizing an amanitin payload. MGTA-117 has potent anti-tumor activity and increases survival in three acute myeloid leukemia (AML) xenograft hNSG mice models (Kasumi-1, AML PDX 1 and AML PDX 2). MGTA-117 enables hematopoietic stem cell transplantation (HSCT) preprocessing in AML, myelodysplasia with excess blasts (MDS-EB) and gene therapy .

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