Bcr-Abl

<p>Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR,</p>

<p>Dasatinib (BMS-354825) is a tyrosine kinase inhibitor that inhibits Src and Bcr-Abl (Ki=16/30 pM) and is orally active and ATP-competitive.</p>

<p>Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.</p>

<p>Nilotinib (AMN107) is a Bcr-Abl tyrosine kinase inhibitor. Nilotinib has antitumor activity and may be used in CML. Cost-effective and quality-assured.</p>

<p>N-Desmethyl imatinib (Imatinib metabolite N-Desmethyl imatinib) is a metabolite of Imatinib, which is a multi-target inhibitor of c-Kit, v-Abl, and PDGFR.</p>

<p>Lyn-IN-1 (Bafetinib analog) is a selective and potent dual inhibitor of Bcr-Abl and Lyn</p>

<p>AKE-72 is a Pan-BCR-ABL inhibitor with anti-leukemic activity.AKE-72 inhibits the proliferation of Ba/F3 cells expressing natural BCR-ABL or its T315I mutant.</p>

<p>LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.Cost-effective and quality-assured.</p>

<p>Dasatinib monohydrate, an oral SRC-kinase inhibitor, counters imatinib-resistant chronic myeloid leukemia.</p>

<p>ML 2-23 is a potent BCR-ABL degrader operating as a PROTAC, exhibiting selective proteasome-dependent degradation of BCR-ABL within leukemia cells [1].</p>

<p>SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).</p>

<p>C-ABL-IN-5, a selective c-Abl inhibitor, exhibits neuroprotective properties and has favorable characteristics including blood-brain barrier permeability,</p>

<p>A unique collection of 263 kinase inhibitors/regulators for specific targeting of kinases, ready for high-throughput screening and high-content screening.</p>

<p>GMB-475 is a PROTAC ligand targeting BCR-ABL1 for degradation via E3 ligase recruitment.</p>

<p>SNIPER(ABL)-047, a compound that links HG-7-85-01 (an ABL inhibitor) to MV-1 (an IAP ligand) via a linker, effectively decreases the BCR-ABL protein levels,</p>

<p>BCR-ABL-IN-3 irreversibly inhibits Bcr-Abl with &lt;100 nM IC50, showing significant anti-cancer effects.</p>

<p>SNIPER(ABL)-020, a Dasatinib-Bestatin conjugate via linker, inhibits ABL and targets IAP, reducing BCR-ABL protein.</p>

<p>SNIPER(ABL)-019, a compound that links Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, exhibiting a</p>

<p>Imatinib impurities3 is a protein kinases inhibitor with IC50 values of 6.95uM, 0.245uM, 0.139uM for ABL1 wt, KIT wt, PDGFRR wt, respectively.</p>

<p>FGFRs-IN-1 (Compound A16) is an orally active inhibitor targeting FGFR1/2/3/4, with IC50 values of 2.3, 7, 11, and 163 nM respectively. It also inhibits VEGFR1/2/3, Abl, and Flt3, with IC50 values of 61, 176, 112, 26, and 353 nM. The compound shows weak inhibition of CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and it inhibits epithelial-mesenchymal transition (EMT) in A549 cells stimulated by TGF-β1. Additionally, FGFRs-IN-1 demonstrates anti-inflammatory activity in mouse models of lung fibrosis induced by Bleomycin and liver fibrosis induced by CCl4.</p>

<p>SNIPER(ABL)-013, a compound that links GNF5 (ABL inhibitor) with Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of</p>

<p>SNIPER(ABL)-015, a compound that conjugates GNF5 (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of 5</p>

<p>SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker.</p>

<p>SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of</p>

<p>SNIPER(ABL)-033, a compound that conjugates HG-7-85-01 (ABL inhibitor) to a LCL161 derivative (IAP ligand) via a linker, effectively reduces BCR-ABL protein</p>

<p>DPH is a potent cell permeable activator of c-Abl. It shows potent enzymatic and cellular activity in stimulating c-Abl activation.</p>

<p>BCR-ABL-IN-9 (Compound B1) is an inhibitor of BCR-ABL that achieves sustained suppression through the formation of stable covalent bonds with the ABL kinase. It effectively inhibits the activity of ABL kinase (IC50 = 1.2 nM) and possesses anticancer activity.</p>

<p>Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI) exhibiting antiproliferative activity against the chronic myeloid leukemia (CML) cell line K562, with a CC50 of 0.8 µM. Tyrosine kinase-IN-8 is applicable for research in chronic leukemia.</p>

<p>AD57 is a potent inhibitor of both c-Src and Abl with IC50 of 0.025 μM and 0.041 μM, respectively.</p>

<p>SNIPER(ABL)-044, a compound that links HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, achieving a</p>

<p>A unique collection of 2720 kinase inhibitors/regulators for high throughput screening and high content screening for drug discovery in kinase related diseases;</p>

<p>A unique collection of 1016 tyrosine kinase inhibitors for high throughput screening and high content screening for drug discovery in tyrosine kinase related</p>

<p>Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ).</p>

<p>SNIPER(ABL)-058, a compound that links Imatinib (ABL inhibitor) with a derivative of LCL161 (IAP ligand) through a linker, effectively decreases BCR-ABL protein</p>

<p>PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, promotes Bcr-Abl degradation through the ubiquitin-proteasome pathway and</p>

<p>cSRC/BCR-ABL-IN-1 (compound 21b) is a potent inhibitor of Bcr-Abl and C-Src, with IC50 values of 56.2 nM and 101 nM, respectively. It exhibits cytotoxicity.</p>

<p>SNIPER(ABL)-049, a compound that conjugates Imatinib (ABL inhibitor) with Bestatin (IAP ligand) through a linker, effectively reduces BCR-ABL protein levels,</p>

<p>BCR-ABL-IN-10 (compound B4) is a covalent BCR-ABL inhibitor featuring an arylvinylsulfonate (AVS) moiety, demonstrating an IC50 of 43.1 nM against ABL kinase. It forms a covalent and stable adduct with ABL kinase, enabling the sustained inhibition of intrinsic BCR-ABL activity. This compound is utilized in the study of chronic myeloid leukemia (CML).</p>

<p>SNIPER(ABL)-024, a compound that conjugates GNF5 (ABL inhibitor) to an LCL161 derivative (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels,</p>

<p>SIAIS100, a potent BCR-ABL PROTAC degrader, demonstrates a DC50 value of 2.7 nM, highlighting its efficacy.</p>

<p>cSRC/BCR-ABL1-IN-1 (compound 16a) is a dual-target inhibitor of the cSRC/BCR-ABL1 kinases.</p>

<p>Asciminib (ABL001) hydrochloride is a selective and potent mutant BCR-ABL1 inhibitor that inhibits Ba/F3 cell growth (IC50: 0.25 nM).</p>

<p>Vodobatinib (K-0706) is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity.</p>

<p>GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.</p>

<p>Degrasyn (WP1130) inhibits DUBs (USP5, UCH-L1, USP9x, USP14, UCH37) and Bcr/Abl without affecting the 20S proteasome.</p>

<p>Nocodazole: synthetic microtubule polymerization blocker, also impedes Abl with low IC50; binds to beta-tubulin.</p>

<p>DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC,</p>

<p>Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively</p>

<p>NVP-BAW2881 (BAW2881) is a potent and selective VEGFR inhibitor with activity to inhibit chronic and acute skin inflammation.</p>

<p>AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).</p>

<p>Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) is a Multi-kinase inhibitor.</p>

<p>Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.</p>

<p>AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM).</p>

<p>Olverembatinib dimesylate (GZD824 Dimesylate) is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).</p>

<p>Dasatinib N-oxide is a key metabolite and potential impurity of the kinase inhibitor dasatinib.</p>

<p>Olverembatinib (GZD 824) is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).</p>

<p>GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.</p>

<p>GMB-475, a PROTAC-based BCR-ABL1 inhibitor, tackles drug resistance by promoting VHL-mediated degradation.</p>

<p>KW-2449 is a multiple-targeted inhibitor, mostly for Flt3, modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.</p>

<p>BGG463 (K 0859) can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with an IC50 of 0.25 μM, 0.09 μM and 0.590 μM, respectively.</p>

<p>Asciminib (ABL001) (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM).</p>

<p>Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit</p>

<p>XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).</p>

<p>Bafetinib (INNO-406): Dual Bcr-Abl/Lyn inhibitor; IC50: 5.8/19 nM; ineffective against T315I mutant, less on c-Kit/PDGFR.</p>

<p>GNF-5, non-ATP Bcr-Abl inhibitor (IC50: 0.22±0.1 uM, wild-type), improves upon GNF-2 with better pharmacokinetics.</p>

<p>Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.</p>

<p>CZC-8004 (CZC-00008004) is a pan-kinase(ABL kinase) inhibitor and binds a range of tyrosine kinases.</p>

<p>Adaphostin (NSC-680410) is a p210Bcr/Abl tyrosine kinase inhibitor with IC50 of 14 μM.</p>

<p>Nilotinib monohydrochloride monohydrate (Nilotinib (monohydrochloride monohydrate)) is significantly potent BCR-ABL against, is a second generation tyrosine</p>

<p>AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.</p>

<p>PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and</p>

<p>Bosutinib hydrate (SKI-606 hydrate) is a kinase inhibitor of BCR-ABL and Src tyrosine kinases for the study of leukemia.</p>

<p>BCR-ABL-IN-7 is an inhibitor of ABL kinase activity in WT and T315I mutants.BCR-ABL-IN-7 can be used in chronic myeloid leukemia (CML) research.</p>

<p>BCR-ABL1-IN-1: potent, orally active ABL kinase inhibitor with high specificity, promising for CNS research.</p>

<p>Debio 0617B inhibits kinases for AML stem cell treatment, targeting JAK, ABL, SRC, and STAT3-related tumours.</p>

<p>Antiproliferative agent-30 (Compound 8g) demonstrates broad-spectrum antiproliferative activity, with IC50 values of 0.054 nM, 0.008 nM, and 0.144 nM against</p>

<p>BCR-ABL-IN-6, an imatinib derivative, inhibits Bcr-AblWT (4.6 nM IC50) and T315I (277 nM), for chronic myeloid leukemia study.</p>

<p>C-ABL-IN-2 is a potent c-Abl protein inhibitor, promising for research in cancer and neurodegenerative diseases like ALS and PD.</p>

<p>AN-019 (NRC-019) is a Bcr-Abl kinase inhibitor with antitumor activity for the study of chronic myelogenous leukemia (CML) and breast cancer.</p>

<p>CHMFL-ABL-053: potent, selective BCR-ABL/SRC/p38 inhibitor (IC50: 70/90/62 nM). Orally available, potential CML drug.</p>

<p>BGB659 is effective inhibitor of RAF.</p>

<p>Tyrphostin AG 568 promotes Tyrphostin-induced inhibition of p210bcr-abl tyrosine kinase activity. It also induces K562 to differentiate.</p>

<p>BCR-ABL-IN-5: Bcr-Abl kinase inhibitor, IC50: Bcr-AblWT 0.014 μM, Bcr-AblT315I 0.45 μM; anti-leukemia cell growth.</p>

<p>AFG210 is a novel first-generation “type II” FLT3 inhibitor.</p>

<p>AP 24149, a potent dual inhibitor targeting Src and Abl, exhibits IC50 values of 9.1 nM for Src and 3.6 nM for Abl, respectively.</p>

<p>CpCDPK1/TgCDPK1-IN-1 is a inhibitor of CpCDPK1 and TgCDPK1, inhibits Abl and Src, and has antiparasitic activity for the study of Toxoplasma infections.</p>

<p>BCR-ABL-IN-2 is a BCR-ABL1 tyrosine kinase inhibitor (IC50s: 57 nM, 773 nM for ABL1 native and ABL1 T315I).</p>

<p>PF-06651481-00 (Bosutinib Isomer I) is a Bosutinib analog and a Bcr-Abl inhibitor.</p>

<p>BCR-ABL-IN-1 is a BCR-ABL tyrosine kinase inhibitor (pIC50: 6.46) and may be used in the research of chronic myelogenous leukemia.</p>

<p>LS-104 is a JAK2 inhibitor.</p>

<p>PD-173956 is an inhibitor of the Src family tyrosine kinases.</p>

<p>PPY A is a potent inhibitor of T315l mutant and wild-type Abl kinase and inhibits the growth of Bcr-Abl T315l mutant or wild-type Bcr-Abl gene-transformed cells</p>

<p>Nilotinib HCl (AMN-107 HCl), an oral Bcr-Abl inhibitor, targets neuroinflammation, cognitive issues, and chronic myelogenous leukemia.</p>

<p>Pivanex, an oral HDAC inhibitor, targets metastasis, angiogenesis, reduces Bcr-Abl protein, and promotes apoptosis.</p>

<p>BCR-ABL-IN-4: Anticancer BCR-ABL inhibitor; stops K562 cells (IC50: 0.67 nM), targets T315I Ba/F3 cells (IC50: 16 nM).</p>

<p>Risvodetinib: potent inhibitor of protein tyrosine kinases c-Abl1, c-Abl2, and c-kit.</p>

<p>CT-721: potent, time-bound Bcr-Abl inhibitor, IC50 21.3 nM, effective against CML.</p>

<p>HG-7-86-01 is a selective type II tyrosine kinase inhibitor with antiproliferative activity against mutant T315I- Bcr-Abl for chronic myeloid leukemia (CML).</p>

<p>Tyrosine kinase-IN-9 (Compound B) is an inhibitor of c-Abl. It is useful for studying neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.</p>

<p>PP487 is a dual tyrosine kinase/PI(3)K inhibitor, exhibiting IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and &lt; 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. It is applicable in cancer research [1].</p>

<p>HSN748 is an analog of ponatinib and acts as a multi-kinase inhibitor. It exhibits inhibitory activity against kinases such as FLT3, ABL1, RET, PDGFRα/β, MNK1, and MNK2. HSN748 can suppress the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines, making it a useful compound in leukemia research.</p>

<p>BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor featuring a trimethoxy group [1].</p>