abl (t315i)

Nocodazole (Oncodazole) is a reversible inhibitor of microtubule polymerization and an inhibitor of Bcr-Abl. Nocodazole has antitumor activity, blocks the cell cycle and induces apoptosis.

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.

Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR ABL and BCR ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease.

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, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.

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).

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).

BGG463 (K 0859) can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.

Bafetinib (INNO-406) (INNO-406) is an effective and specific dual Bcr-Abl Lyn inhibitor (IC50: 5.8 19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR.

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

GZD856 is an orally bioavailable PDGFRα β inhibitor (IC50s: 68.6 and 136.6 nM) with anti-lung cancer activities.

DB07107 is a potent inhibitor of drug resistant T315I mutant Bcr-Abl tyrosine kinase and a potent Akt1 inhibitor (IC50: 360 nM).

AT-9283 L-lactate is an inhibitor of aurora kinase.

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

MPT0B002 is a microtubule inhibitor that acts by downregulating T315I mutant Bcr-Abl and inducing apoptosis of imatinib-resistant chronic myeloid leukemia cells.

HS-438 inhibits imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia.

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

HG-7-85-01 is a novel ATP-competitive and type II tyrosine kinase inhibitor targeting both wild-type and watchman mutant BCR-ABL, PDGFRα, Kit, and Src kinases, with inhibitory effects on the proliferation of a variety of cancer cell lines, leading to G0 G1-phase blockade and apoptosis induction in BCR-ABL-expressing cells.

BV02 is an inhibitor of 14-3-3 protein-protein interactions and can be used in studies about the treatment of chronic myeloid leukemia. BV02 disrupts hematopoietic cells expressing the IM-resistant T315I mutation and the IM-sensitive wild-type Bcr-Abl.

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

c-ABL-IN-4, a potent inhibitor of c-Abl, exhibits strong activity in inhibiting the Bcr-Abl (IC50 = 4.5 nM) kinase activity and proliferation (IC50 = 0.41-2.12 μM) of Bcr-Abl(T315I) cell lines.

BCR-ABL-IN-4 is a BCR-ABL inhibitor exhibiting anticancer activity with an inhibitory effect on cancer cell growth, specifically on K562 cells (IC50: 0.67 nM) and BCR-ABL T315I-transfected Ba F3 cells (IC50: 16 nM).

GZD856 formic is a potent, orally active inhibitor of PDGFRα β and Bcr-Abl T315I, demonstrating IC50 values of 68.6 nM and 136.6 nM for PDGFRα β, respectively, and 19.9 nM and 15.4 nM for native Bcr-Abl and the T315I mutant, respectively. This compound exhibits significant antitumor activity.

AKI603 is a novel small molecule inhibitor of Aurora kinase A (AurA)(IC50 = 12.3 nM). AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells[1][2].

AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the low nanomolar cellular and biochemical inhibitory properties of AP23464 extend to frequently observed imatinib mesylate-resistant Bcr-Abl mutants, including nucleotide binding P-loop mutants Q252H, Y253F, E255K, C-terminal loop mutant M351T, and activation loop mutant H396P. AP23464 was ineffective against mutant T315I, an imatinib mesylate contact residue. The potency of AP23464 against imatinib mesylate-refractory Bcr-Abl and its distinct binding mode relative to imatinib mesylate warr......