Bcr-Abl
Bcl-Abl is a constitutively activated chimeric tyrosine kinase which is the genetic abnormality expressed in patient with CML (chronic myeloid leukemia).
Products for Bcr-Abl
- Cat.No. Product Name Information
- GC12172 1-Naphthyl PP1 Src family kinases inhibitor
- GC15579 Adaphostin P210bcr/abl tyrosine kinase inhibitor
- GC32703 Asciminib (ABL001) Asciminib (ABL001) (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
- GC64462 Asciminib hydrochloride Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
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GC35462
Bafetinib
Bcr-Abl/Lyn tyrosine kinase inhibitor
- GC33343 BCR-ABL-IN-1 BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
- GC33368 BCR-ABL-IN-2 BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.
- GC13343 Bosutinib (SKI-606) Bosutinib (SKI-606) is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.
- GC40080 Bosutinib-d8 Bosutinib-d8 is intended for use as an internal standard for the quantification of bosutinib by GC- or LC-MS.
- GC35651 Cenisertib Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
- GC35682 CHMFL-ABL/KIT-155 CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
- GC35753 CT-721 CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities.
- GC33351 CZC-8004 (CZC-00008004) CZC-8004 (CZC-00008004) (CZC-00008004), an aminopyrimidine, is a pan-kinase inhibitor. CZC-8004 (CZC-00008004) can bind a range of tyrosine kinases, including EGFR and VEGFR2 with IC50 values of 650 and 437 nM, respectively.
- GC35812 Dasatinib hydrochloride A potent and dual AblWT/Src inhibitor
- GC15884 Dasatinib Monohydrate Inhibitor of ABL, SRC, KIT, PDGFR, and other tyrosine kinases.
- GC14007 DCC-2036 (Rebastinib) DCC-2036 (Rebastinib) (DCC-2036) is an orally active, non-ATP-competitiveBcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50s of 0.8 nM and 4 nM, respectively. DCC-2036 (Rebastinib) also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
- GC35897 DPH A potent cell permeable c-Abl activator
- GC32867 Flumatinib (HHGV678) Flumatinib (HHGV678) (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib (HHGV678) inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
- GC13914 Flumatinib mesylate PDGRFβ inhibitor
- GC36167 GMB-475 GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
- GC10858 GNF 2 Bcr-Abl inhibitor
- GC15079 GNF 5 Bcr-Abl inhibitor
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GC10607
GNF-7
Type II Bcr-Abl inhibitor
- GC10915 GZD824 Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity.
- GC33201 GZD856 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-AblT315I inhibitor, with IC50s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
- GC10314 Imatinib (STI571) Imatinib (STI571) (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib (STI571) also is an inhibitor of SARS-CoV and MERS-CoV.
- GC11759 Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
- GC25669 Nilotinib hydrochloride Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
- GC14075 Nocodazole A tubulin production inhibitor,anti-neoplastic agent
- GC36807 ON 146040 ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
- GC12637 PD 180970 P210bcr/abl tyrosine kinase inhibitor
- GC13592 PD173955 Dual Src/Abl kinase inhibitor, ATP-competitive,
- GC14396 Ponatinib (AP24534) Ponatinib (AP24534) (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
- GC45828 Ponatinib-d8 An internal standard for the quantification of ponatinib
- GC12779 PPY A Abl kinases inhibitor
- GC11140 Radotinib(IY-5511) Bcr-Abl tyrosine kinase inhibitor
- GC15197 Saracatinib (AZD0530) Saracatinib (AZD0530) (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib (AZD0530) shows high selectivity over other tyrosine kinases.
- GC65592 SNIPER(ABL)-020 SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.
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GC70110
Vamotinib
Vamotinib (PF-114) is an effective, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the self-phosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib exhibits anti-proliferative and anti-tumor activity. Vamotinib has potential in the study of resistant Philadelphia chromosome-positive (Ph+) leukemia.
- GC10970 WP1130 WP1130 (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. WP1130 has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.