Search Result

Results for "

acute leukemia xenograft model

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Antibody (1) Akt (1) Apoptosis (12) Atg8/LC3 (3) Autophagy (3) Bcl-2 Family (3) Casein Kinase (1) Caspase (4) CD3 (1) CDK (1) Ceramidase (1) Checkpoint Kinase (Chk) (1) ClpP (1) CXCR (1) Epigenetic Reader Domain (4) Eukaryotic Initiation Factor (eIF) (1) Fat Mass and Obesity-associated Protein (FTO) (1) FLT3 (3) Histone Acetyltransferase (1) HIV (1) HSP (1) IKZF Family (1) Interleukin Related (2) JAK (4) LPL Receptor (1) MDM-2/p53 (3) mTOR (1) NF-κB (1) Notch (2) p38 MAPK (1) p62 (3) p97 (1) PARP (1) PERK (1) PI3K (1) PROTACs (5) Reactive Oxygen Species (ROS) (3) RET (1) Small Interfering RNA (siRNA) (1) STAT (5) Wee1 (1)
By Research Areas:	Cancer (30) Cardiovascular Disease (3) Inflammation/Immunology (3) Neurological Disease (1)

By Targets:

ADC Antibody (1)

Akt (1)

Apoptosis (12)

Atg8/LC3 (3)

Autophagy (3)

Bcl-2 Family (3)

Casein Kinase (1)

Caspase (4)

CD3 (1)

CDK (1)

Ceramidase (1)

Checkpoint Kinase (Chk) (1)

ClpP (1)

CXCR (1)

Epigenetic Reader Domain (4)

Eukaryotic Initiation Factor (eIF) (1)

Fat Mass and Obesity-associated Protein (FTO) (1)

FLT3 (3)

Histone Acetyltransferase (1)

HIV (1)

HSP (1)

IKZF Family (1)

Interleukin Related (2)

JAK (4)

LPL Receptor (1)

MDM-2/p53 (3)

mTOR (1)

NF-κB (1)

Notch (2)

p38 MAPK (1)

p62 (3)

p97 (1)

PARP (1)

PERK (1)

PI3K (1)

PROTACs (5)

Reactive Oxygen Species (ROS) (3)

RET (1)

Small Interfering RNA (siRNA) (1)

STAT (5)

Wee1 (1)

By Research Areas:

Cancer (30)

Cardiovascular Disease (3)

Inflammation/Immunology (3)

Neurological Disease (1)

Inhibitors & Agonists

Inhibitory Antibodies

Targets Recommended: BMI1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-174979

Dac590	Fat Mass and Obesity-associated Protein (FTO) Apoptosis	Cancer
Dac590 is an orally active FTO inhibitor. Dac590 has a robust antiproliferative effect on AML cells, and induces apoptosis and cell cycle G1 arrest by inhibiting oncogenic FTO signaling. Dac590 significantly inhibits tumor growth and prolongs survival with no observed toxicity in acute myeloid leukemia (AML) xenograft mcie model, and shows a synergistic effect combined with Decitabine (HY-A0004) .

HY-148422

Rohinitib 1 Publications Verification	Eukaryotic Initiation Factor (eIF) Apoptosis	Cancer
Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .

HY-P99272

Ulocuplumab 1 Publications Verification BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody	CXCR	Cancer
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .

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-133760

MI-888	MDM-2/p53	Cancer
MI-888 is an orally active MDM2 inhibitor with a K_i of 0.44 nM. MI-888 can inhibit the MDM2-p53 interaction. MI-888 has favorable pharmacokinetic properties and anti-tumor activity .

HY-149539

PLM-101	FLT3 RET	Cancer
PLM-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) .

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-155556

ZG36	ClpP	Cancer
ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .

HY-114162B

VTP50469 mesylate	Epigenetic Reader Domain Apoptosis	Cancer
VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.

HY-120372

BMS-871	Notch	Cancer
BMS-871 is an orally active pan-Notch inhibitor with IC₅₀ values of 4/1/4/3 nM for Notch1/2/3/4, respectively. BMS-871 significantly inhibited the proliferation of TALL-1 and MDA-MB-157 cells and demonstrated significant antitumor activity in T-acute lymphoblastic leukemia and triple-negative breast cancer xenograft models. BMS-871 can be used to study leukemia and breast cancer .

HY-148813

AK-2292	PROTACs STAT	Cancer
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC₅₀ of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-154984

JET-209	Histone Acetyltransferase PROTACs	Cancer
JET-209 is a potent CBP/p300 PROTAC degrader, with DC₅₀ values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia (Pink: CBP/p300 ligand (HY-175620); Blue: CRBN ligand (HY-132248); Black: Linker; CBP/p300 ligand + Linker (HY-175621)) .

HY-169937

(R)-SR-C-107	Epigenetic Reader Domain	Cancer
(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC₅₀ and K_D of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .

HY-P99623

Flotetuzumab MGD006; S80880	CD3	Cancer
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .

HY-15815

Bromosporine 4 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-P991328

MAb604.107	Notch	Cancer
MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .

HY-176457

ZS3-046	Small Interfering RNA (siRNA) MDM-2/p53 PROTACs	Cancer
ZS3-046 is a TAF1 PROTAC degrader. ZS3-046 promotes the ubiquitination and degradation of TAF1. ZS3-046 activates p53 and induces apoptosis in acute myeloid leukemia (AML) cells. ZS3-046 has antitumor activity in an AML tumor xenograft mouse model. (Target protein ligand (HY-176467); CRBN ligase (HY-41547); Linker (HY-176469); CRBN ligase + Linker (HY-176470)) .

HY-175783

MM927	Apoptosis	Cancer
MM927 is a potent NVL inhibitor, with an IC₅₀ of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC) .

HY-P991669

IGN523	Caspase Apoptosis	Cancer
IGN523 is an anti-CD98 antibody (hCD98, K_D = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .

HY-158783

SACLAC	Ceramidase Bcl-2 Family LPL Receptor Apoptosis	Neurological Disease
SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a K_i of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .

HY-139901

Chk1-IN-6	Checkpoint Kinase (Chk)	Cancer
Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC₅₀ of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma .

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-174458

MD-4251	PROTACs MDM-2/p53 IKZF Family Casein Kinase	Cancer
MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC₅₀: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker

HY-173320

HEMTAC WEE1 degrader-1	Wee1 HSP	Cancer
HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC₅₀: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .

HY-155066

FD274	PI3K mTOR Apoptosis	Cancer
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC₅₀s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .

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-P99395

Talacotuzumab 1 Publications Verification JNJ 56022473; CSL 362	Interleukin Related	Cancer
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has K_Ds of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .

HY-13559A

Atiprimod dimaleate Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate	STAT Apoptosis Caspase Interleukin Related Autophagy Reactive Oxygen Species (ROS) Atg8/LC3 p62 JAK	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) (dimaleate) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

HY-13559

Atiprimod Azaspirane ; SKF 106615-12; SKF 106615A12	STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Bcl-2 Family p62 Atg8/LC3 PARP NF-κB PERK JAK	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

HY-110102

Atiprimod hydrochloride Azaspirane hydrochloride; SKF 106615-12 hydrochloride; SKF 106615	JAK STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Atg8/LC3 p62	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

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)) .

Cat. No.	Product Name	Target	Research Area