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MV4-11 xenograft model

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-159657
    PF-07899895

    		Salt-inducible Kinase (SIK) Interleukin Related Inflammation/Immunology
    PF-07899895 (Compound 34) is a SIK inhibitor, with IC50 values of 1.2 nM, 0.9 nM, and 1.8 nM against SIK1, SIK2, and SIK3, respectively. PF-07899895 modulates the anti-inflammatory cytokine IL-10 in immune cells. PF-07899895 is applicable to research related to inflammatory diseases .
    PF-07899895
  • HY-155489
    DDO-2728
    2 Publications Verification

    		 Anaplastic lymphoma kinase (ALK) Apoptosis Cancer
    DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4 11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
    DDO-2728
  • HY-171792
    BMS-986497

    ORM-6151

    		 Transmembrane Glycoprotein Cancer
    BMS-986497 (ORM-6151) is a CD33-targeting antibody-conjugated GSPT1 degrader. BMS-986497 delivers the GSPT1 degrader SMol006 to CD33-expressing cells and induces GSPT1 protein degradation. BMS-986497 shows potential for research on acute myeloid leukemia (AML) .
    BMS-986497
  • HY-176428
    PROTAC MNK1 degrader-1

    P11-2

    		 PROTACs MNK Apoptosis Eukaryotic Initiation Factor (eIF) Cancer
    PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety . Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
    PROTAC MNK1 degrader-1
  • 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 .
    Chk1-IN-6
  • HY-162651
    PROTAC BRD9 Degrader-8

    		PROTACs Epigenetic Reader Domain Apoptosis Cancer
    PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma .
    PROTAC BRD9 Degrader-8
  • HY-156566
    PROTAC BRD4 Degrader-21

    		PROTACs Epigenetic Reader Domain HSP Cancer
    PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma .
    PROTAC BRD4 Degrader-21
  • HY-157213
    LWY713

    		Apoptosis PROTACs FLT3 Cancer
    LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
    LWY713
  • HY-174302
    PIM-1/HDAC-IN-2

    		Pim HDAC PARP Apoptosis Cancer
    PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
    PIM-1/HDAC-IN-2
  • 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)) .
    PROTAC FLT3/JAK2/BRD4 Degrader-1
  • 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 .
    HSB401
  • HY-146615
    Axl-IN-6

    		TAM Receptor Cancer
    Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
    Axl-IN-6
  • HY-169075
    CDK/HDAC-IN-4

    		HDAC CDK Apoptosis Cancer
    CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
    CDK/HDAC-IN-4
  • 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%) .
    FLT3-IN-21
  • HY-157295
    PI3K/HDAC-IN-3

    		PI3K HDAC Cancer
    PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC50 values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .
    PI3K/HDAC-IN-3
  • HY-179272
    Wee1/HDAC-IN-1

    		Wee1 HDAC Apoptosis Cancer
    Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC50 of 1.2 nM for Wee1 and IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC50 of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML) .
    Wee1/HDAC-IN-1
  • 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) .
    PLM-101
  • 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) .
    CDK9-IN-19
  • HY-144777
    FLT3-IN-14

    		FLT3 Apoptosis Cancer
    FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
    FLT3-IN-14
  • HY-172399
    FTO-IN-14

    		Fat Mass and Obesity-associated Protein (FTO) Apoptosis Cancer
    FTO-IN-14 (Compound F97) is the inhibitor for the RNA demethylase Fat mass and obesity-associated protein FTO with IC50 of 0.45 μM. FTO-IN-14 regulates the protein expression of ASB2, RARA and MYC. FTO-IN-14 exhibits antiproliferative activity in AML cancer cells (IC50 for MOLM13, NB4, HEL, OCI-AML3, MV4-11 and MONOMAC6 is 0.7-5.5 μM), induces apoptosis in NB4 cell. FTO-IN-14 exhibits antitumor activity in mouse NB4 xenograft models .
    FTO-IN-14
  • 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) .
    FLT3-IN-32 hydrochloride
  • HY-181854
    ZX079

    		PROTACs Epigenetic Reader Domain Histone Acetyltransferase c-Myc Caspase Apoptosis Cancer
    ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC50 value of 0.035 nM and a CBP DC50 value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia .
    ZX079
  • HY-180430
    Antitumor agent-208

    		Drug Derivative Cancer
    Antitumor agent-208, a Bufalin (HY-N0877) analogue, is a potent and orally active antitumor agent. Antitumor agent-208 exhibits antiproliferative activity against tumor cell line (IC50 =0.30-1.09 nM). Antitumor agent-208 inhibits tumor growth in a MV-4-11 xenograft mouse model. Antitumor agent-208 can be used for cancer research, such as acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC) .
    Antitumor agent-208
  • HY-182813
    MC-amide-C2-amide-(β-D-GlcUA)-amide-PEG1-CH2-CC-885

    		Drug-Linker Conjugates for ADC Cancer
    MC-amide-C2-amide-(β-D-GlcUA)-amide-PEG1-CH2-CC-885 is a Drug-Linker Conjugates for ADC composed of CC-885 (HY-101488) and a linker. MC-amide-C2-amide-(β-D-GlcUA)-amide-PEG1-CH2-CC-885 conjugates with GemtUZUmab (HY-P99971) to synthesize an ADC (Compound ADC-2). ADC-2 exhibits anti-tumor activity in a leukemia MV-4-11 xenograft model .
    MC-amide-C2-amide-(β-D-GlcUA)-amide-PEG1-CH2-CC-885
  • HY-182937
    FLC-8

    		FLT3 STAT Akt ERK Caspase PARP Bcl-2 Family Apoptosis Cancer
    FLC-8 is an orally active FLT3 inhibitor with IC50 values of 10.2 nM, 11.6 nM and 24.10 nM against human FLT3-WT, FLT3-G697R and FLT3-N676D, respectively. FLC-8 inhibits FLT3 autophosphorylation and downstream STAT5, AKT and ERK signaling pathways, and induces apoptosis in acute myeloid leukemia (AML) cells. FLC-8 exhibits potent antitumor activity in the MV4-11 xenograft model. FLC-8 can be used for the research of acute myeloid leukemia .
    FLC-8
  • HY-184211
    BRD9 ligand-14

    		Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    BRD9 ligand-14 is a BRD9 ligand that acts as a protein-of-interest ligand for synthesis of BRD9 PROTAC degraders. BRD9 ligand-14 can be used for research in acute myeloid leukemia .
    BRD9 ligand-14
  • HY-183354
    HLC40

    		Histone Methyltransferase WDR5 Apoptosis Caspase Cancer
    HLC40 is a MLL1 histone methyltransferase inhibitor with an IC50 of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model .
    HLC40
  • HY-181867
    PROTAC BET Degrader-16

    		PROTACs Epigenetic Reader Domain Apoptosis Cancer
    PROTAC BET Degrader-16 (Compound A10) is a BET PROTAC degrader with a DC50 of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia .
    PROTAC BET Degrader-16
  • HY-181869
    PROTAC BET Degrader-17

    		PROTACs Epigenetic Reader Domain Apoptosis Cancer
    PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC50=0.09 nM) and BRD4 (IC50=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia .
    PROTAC BET Degrader-17

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