2. Search Result
Search Result
Results for "

T315I Bcr-Abl

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

1

GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13024
    Rebastinib
    Maximum Cited Publications
    12 Publications Verification

    DCC-2036

    		 Bcr-Abl FLT3 Src Apoptosis Cancer
    Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1 WT and Abl1 T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
    Rebastinib
  • HY-15666
    Olverembatinib
    5+ Cited Publications

    GZD824; HQP1351

    		 Bcr-Abl Cancer
    Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity . Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Olverembatinib
  • HY-147414
    Vamotinib

    PF-114

    		 Bcr-Abl Cancer
    Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABL T315I), 9.5 nM (ABL E255K), 2.0 nM (ABL F317I), 7.4 nM (ABL G250E), 1.0 nM (ABL H396P), 2.8 nM (ABL M351T), 12 nM (ABL Q252H), and 4.1 nM (ABL Y253F), respectively . Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Vamotinib
  • HY-10943
    GNF-7
    2 Publications Verification

    		 Bcr-Abl Ack1 Cancer
    GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-Abl WT and Bcr-Abl T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies .
    GNF-7
  • HY-137460
    Vodobatinib
    2 Publications Verification

    K0706

    		 Bcr-Abl Cancer
    Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research . Vodobatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Vodobatinib
  • HY-15666A
    Olverembatinib dimesylate
    5+ Cited Publications

    GZD824 dimesylate; HQP1351 dimesylate

    		 Bcr-Abl Cancer
    Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity . Olverembatinib (dimesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Olverembatinib dimesylate
  • HY-123159
    AKI603

    		Aurora Kinase Cancer
    AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .
    AKI603
  • HY-101985
    BV02
    3 Publications Verification

    		 Bacterial PARP Caspase Apoptosis Autophagy Akt Infection Neurological Disease Inflammation/Immunology
    BV02 is a 14-3-3 inhibitor and an antibacterial agent. BV02 enhances the cleavage of PARP and caspase-3. BV02 induces Apoptosis, Autophagy, and enhances Akt activation. BV02 has anti-B. melitensis infection and epilepsy-promoting effects. BV02 can also be used in colitis research.
    BV02
  • HY-123450
    S116836

    		Bcr-Abl Apoptosis PDGFR Cancer
    S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    S116836
  • HY-101489A
    GZD856 formic

    		PDGFR Bcr-Abl Apoptosis Cancer
    GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity . GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GZD856 formic
  • HY-15814
    HG-7-85-01

    		Bcr-Abl PDGFR c-Kit Src JAK Apoptosis Cancer
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
    HG-7-85-01
  • HY-118144
    PD166326

    		Src Bcr-Abl p38 MAPK Cancer
    PD166326 is an orally active tyrosine kinase inhibitor with a IC50 of 8 nM against abl tyrosine kinase and a IC50 of 6 nM against src tyrosine kinase. PD166326 blocks Bcr/Abl kinase activity. PD166326 inhibits Bcr/Abl-dependent proliferation and cell cycle progression. PD166326 reduces peripheral blood granulocytosis, alleviates splenomegaly and prolongs survival in a mouse model of chronic myeloid leukemia. PD166326 can be used in research related to chronic myeloid leukemia .
    PD166326
  • HY-164393
    ON044580

    		JAK Bcr-Abl Apoptosis Cancer
    ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
    ON044580
  • HY-101489
    GZD856

    		PDGFR Bcr-Abl Apoptosis Cancer
    GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity .
    GZD856
  • HY-18819
    BCR-ABL-IN-2

    		Bcr-Abl Cancer
    BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1 native and ABL1 T315I, respectively.
    BCR-ABL-IN-2
  • HY-10364
    AP24163

    		Bcr-Abl Cancer
    AP24163 is a BCR-ABL kinase inhibitor. AP24163 inhibits wild-type (native) BCR-ABL and BCR-ABL-T315I with IC50 values of 7 nM and 511 nM, respectively. AP24163 can be used in the research of chronic myeloid leukemia (CML) .
    AP24163
  • HY-15666R
    Olverembatinib (Standard)

    GZD824 (Standard); HQP1351 (Standard)

    		 Reference Standards Bcr-Abl Cancer
    Olverembatinib (Standard) is the analytical standard of Olverembatinib. This product is intended for research and analytical applications. Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity . Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Olverembatinib (Standard)
  • HY-176269
    VS1150

    		Bcr-Abl ERK STAT PARP Caspase Apoptosis Cancer
    VS1150 (Compound 11) is a BCR-ABL-targeting phosphorylation-inducing chimeric small molecule (PHICS). VS1150 significantly inhibits oncogenic kinase BCR-ABL signaling by inducing inhibitory phosphorylation at its Y253 (EC50: 69 nM), subsequently triggering cell apoptosis. VS1150 also inhibits other oncogenic ABL fusions and drug-resistant mutants like T315I. VS1150 can be used for chronic myeloid leukemia (CML) and other ABL fusion-driven cancers research .
    VS1150
  • HY-153008
    BCR-ABL-IN-7

    		Bcr-Abl Cancer
    BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research .
    BCR-ABL-IN-7
  • HY-142922
    BCR-ABL-IN-4

    		Bcr-Abl Cancer
    BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11) .
    BCR-ABL-IN-4
  • HY-E70640
    ABL1 T315I Recombinant Human Active Protein Kinase

    		Bcr-Abl Cancer
    The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 T315I Recombinant Human Active Protein Kinase is a recombinant ABL1 T315I protein that can be used to study ABL1 T315I-related functions .
    ABL1 T315I Recombinant Human Active Protein Kinase
  • HY-123390
    DB07107

    		Bcr-Abl Akt Cancer
    DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM .
    DB07107
  • HY-160478
    GNF-6

    		Bcr-Abl Cancer
    GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
    GNF-6
  • HY-180981
    P19As

    		PROTACs Bcr-Abl Cancer
    P19As is a BCR-ABL PROTAC degrader based on Asciminib (HY-104010), with a DC50 value of approximately 200 nM for the wild-type BCR-ABL protein. P19As can degrade the T315I mutant and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19As can be used for the study of chronic myeloid leukemia and acute lymphoblastic leukemia .
    P19As
  • HY-180979
    P22D

    		PROTACs Bcr-Abl Cancer
    P22D is a BCR-ABL PROTAC degrader based on Dasatinib (HY-10181), with a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. P22D cannot degrade the BCR-ABL T315I mutant. P22D has inhibitory activity against K562 cells (wild type), but is ineffective against BaF3-BCR-ABL (T315I) cells. P22D can be used for research on chronic myeloid leukemia and acute lymphocytic leukemia .
    P22D
  • HY-180977
    P19P

    		PROTACs Bcr-Abl Cancer
    P19P is a BCR-ABL PROTAC degrader based on Ponatinib (HY-12047), with a DC50 value of approximately 20 nM for the wild-type BCR-ABL protein. P19P can effectively degrade various drug-resistant mutants such as T315I, E255K, H396R, and V468F, and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19P maintains strong inhibitory activity against ABL (T315I), with a IC50 of 13.1 nM. P19P does not inhibit the formation of vascular lumens in HUVEC. P19P can be used for research on chronic myeloid leukemia and acute lymphoblastic leukemia .
    P19P
  • HY-165532
    SGX393

    SGX70393

    		 Bcr-Abl Cancer
    SGX393 (SGX70393) is a Bcr-Abl kinase inhibitor. SGX393 binds to the active conformation of the kinase domains of both wild-type and T315I mutant Bcr-Abl, thereby inhibiting kinase activity. SGX393 exhibits antiproliferative effects in cells expressing wild-type or T315I mutant Bcr-Abl, and suppresses T315I-driven tumor growth. SGX393 can be used for the research of chronic myeloid leukemia .
    SGX393
  • HY-177273
    Kinase modulator-1

    		Bcr-Abl Cancer
    Kinase modulator-1 (P142, MS: m/z445) is a kinase modulator. Kinase modulator-1 can inhibit Bcr-Abl activity, especially against drug-resistant mutant kinases (such as T315I Bcr-Abl). Kinase modulator-1 can be used for cancers like chronic myelogenous leukemia (CML) research .
    Kinase modulator-1
  • HY-112404
    BCR-ABL-IN-13

    		Src Bcr-Abl Cancer
    BCR-ABL-IN-13 is a dual c-Src and Abl inhibitor, with a Ki value of 0.55 μM against c-Src, 0.10 μM against wild-type Abl, and 0.40 μM against the Abl T315I mutant. BCR-ABL-IN-13 exerts competitive/mixed-type inhibitory effects on wild-type Abl, and non-competitive inhibitory effects on the drug-resistant Abl T315I mutant. BCR-ABL-IN-13 can be used for the research of chronic myeloid leukemia .
    BCR-ABL-IN-13
  • HY-164469
    CHMFL-48

    		Bcr-Abl Apoptosis STAT Cancer
    CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML) .
    CHMFL-48
  • HY-157389
    AK-HW-90

    		Bcr-Abl Cancer
    AK-HW-90 (compound 2B) is a potent panBcr-Abl inhibitor with significant inhibitory activity against Imatinib (HY-15463)-resistant mutants. AK-HW-90 inhibits the resistance mutant Bcr-Abl T315I with an IC50 of 0.65 nM. AK-HW-90 has potential anticancer activity and can be used in the study of chronic myelogenous leukemia (CML) .
    AK-HW-90
  • HY-10212A
    BIIB021 mesylate

    CNF2024 mesylate

    		 HSP β-catenin c-Myc Autophagy Cancer
    BIIB021 (CNF2024) mesylate is the mesylate of BIIB021 (HY-10212). BIIB021 is an orally active Hsp90 inhibitor. BIIB021 inhibits the proliferation of chronic myeloid leukemia (CML) cells, with IC50 values of K562, K562/G, 32Dp210, and 32Dp210-T315I cells are 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 degrades BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. BIIB021 can also induce autophagy in CML cells. BIIB021 can be used for the research of CML .
    BIIB021 mesylate
  • HY-180967
    PROTAC BCR-ABL Degrader-2

    		Bcr-Abl PROTACs Apoptosis Cancer
    PROTAC BCR-ABL Degrader-2 is a selective Bcr-Abl T315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-Abl T315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research .
    PROTAC BCR-ABL Degrader-2
  • HY-12292G
    IM-12

    		NF-κB STAT GSK-3 β-catenin Bcr-Abl Cancer
    IM-12 GMP is IM-12 (HY-12292) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. IM-12 is an orally active anti-inflammatory agent that targets and inhibits the NF-κB and STAT3 signaling pathways. IM-12 activates the Wnt signaling pathway and promotes the nuclear translocation of β-catenin by inhibiting GSK3β, while also blocking the tyrosine kinase activity of p210BCR/ABL. IM-12 reduces the levels of IL-6, IL-17, NO, prostaglandin E2, iNOS and COX-2, and induces ER stress, Ca 2+ release, autophagy and apoptosis. IM-12 is heat-sensitive and does not induce autophagy in IM-resistant p210BCR/ABL T315I mutant cells. IM-12 is also a component of the 5iLA medium used for naive pluripotent stem cell research. IM-12 has been applied in studies related to carrageenan (HY-125474)-induced hind paw edema, TNBS-induced colitis, and acute and chronic myeloid leukemia .
    IM-12
  • HY-101985R
    BV02 (Standard)

    		Reference Standards Bacterial PARP Caspase Apoptosis Autophagy Akt Infection Neurological Disease Inflammation/Immunology
    BV02 (Standard) is the analytical standard of BV02 (HY-101985). This product is intended for research and analytical applications. BV02 is a 14-3-3 inhibitor and an antibacterial agent. BV02 enhances the cleavage of PARP and caspase-3. BV02 induces Apoptosis, Autophagy, and enhances Akt activation. BV02 has anti-B. melitensis infection and epilepsy-promoting effects. BV02 can also be used in colitis research.
    BV02 (Standard)

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: