Bcr-Abl

An internal standard for the quantification of ponatinib

Imatinib-d3 (STI571-d3) hydrochloride is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (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 also is an inhibitor of SARS-CoV and MERS-CoV.

An inhibitor of MAP4K2 and TAK1

A neuropeptide with diverse biological activities

Ponatinib (hydrochloride) is a multi-target tyrosine kinase inhibitor that inhibits the activity of Abl (IC₅₀=0.37nM), PDGFRα (IC₅₀=1.1nM), VEGFR2 (IC₅₀=1.5nM), FGFR1 (IC₅₀=2.2nM), and Src (IC₅₀=5.4nM).

An internal standard for the quantification of nilotinib

Imatinib D4 (STI571 D4) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity.

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.

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-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity.

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.

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.

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.

SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.

Lyn-IN-1 (Bafetinib analog) is a highly active dual inhibitor of Bcr-Abl and Lyn.

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.

HG-7-86-01 (Compound 26) is type II tyrosine kinase inhibitor.

PD173952 is a tyrosine kinases inhibitor with IC50s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively.

Risvodetinib (IkT-148009) is an oral, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM.

SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM.

PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoetl linker.

BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group.

AKE-72 (compound 5) is a potent inhibitor of Pan-BCR-ABL.

Asciminib-NH2 is a BCR-ABL ligand and can be used for the synthesis of PROTACs, such as P19As [1] .

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.