Bcr-Abl

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,

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.

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

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.

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.

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.

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.

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

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

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.

SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner in K562 cells and reduces the phosphorylation levels of BCR-ABL and its downstream molecules, STAT5 and CRKL. SIAIS056 can induce the degradation of various clinically relevant BCR-ABL resistant mutants and exhibits antiproliferative activity against K562 and 32D-BCR-ABL cells. Additionally, it can cause significant tumor regression in K562 xenograft models and is applicable for leukemia research.

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

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

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

P19As is a BCR-ABL PROTAC degrader based on Asciminib, with a DC50 of approximately 200 nM for the wild-type BCR-ABL protein. It is capable of degrading the T315I mutant and demonstrates strong antiproliferative activity in BaF3-BCR-ABL (T315I) cells. P19As is applicable for research in chronic myeloid leukemia and acute lymphoblastic leukemia.

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

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.

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

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].

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