imatinib-resistant

AKI603 是一种极光激酶 A 抑制剂，IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性，可用于克服白血病中 BCR-ABL-T315I 耐药性突变。

Nilotinib (AMN107) 是一种 Bcr-Abl 酪氨酸激酶抑制剂，具有口服活性。Nilotinib 具有抗肿瘤活性，可以用于治疗 Imatinib 耐药的慢性粒细胞性白血病 (CML)。

Anticanceragent 259 (Compound 3g) 是Telmisartan衍生的细胞死亡调节剂，能够干扰STAT5信号通路，提高Imatinib在耐药细胞中的敏感性，SC50为1.5 μM。

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.

PPARγ agonist 3, also known as Compound 18a, is a potent and selective agonist of PPARγ. This compound does not exhibit cytotoxicity towards both non-resistant and resistant cells. Notably, PPARγ agonist 3 demonstrates antitumor efficacy exclusively when co-administered with Imatinib [1].

PPARγ agonist 4 (Compound 18b), a potent and selective PPARγ agonist, demonstrates antitumor efficacy only when used in conjunction with Imatinib. Notably, PPARγ agonist 4 does not exhibit cytotoxic effects on either non-resistant or resistant cells [1].

Nilotinib hydrochloride dihydrate is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia.

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......

ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I.

PHA-680626 is a potent and selective PLK inhibitor. PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases. PHA-680626 inhibits Plk1 (IC50 = 0.53 μM), Plk2 (IC50 = 0.07 μM) and Plk3 (IC50 = 1.61 μM).

Nilotinib dihydrochloride dihydrate is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia.

Nilotinib N-oxide is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia.

Berbamine acetate (Compound 3a) 是 Berbamine 的衍生物，具有抗肿瘤活性，能够抑制对 Imatinib 耐药的 K562 白血病细胞的生长，IC50 为 6.6 μM。

ON044580,一种α-苯甲酰苯乙烯基苄基硫醚类化合物,作为非ATP竞争性的JAK2抑制剂,对WT和V617F突变型JAK2显示出较低的IC50,分别为1.23 μM和1.09 μM.该化合物抑制JAK2激酶活性,主要通过与STAT-5结合域或变构位点结合实现.ON044580能够在JAK2V617F阳性的白血病细胞中抑制细胞增殖,并能有效诱导对Imatinib耐药的慢性粒细胞白血病(CML)细胞的凋亡.此外,ON044580也能抑制BCR-ABL激酶的WT及T315I突变形式,是研究以异常JAK STAT信号为特征的骨髓增生性疾病的有力工具.

CHMFL-48是一种对BCR-ABL激酶（包括野生型(wt)及多种耐Imatinib突变体）具有口服活性的抑制剂。CHMFL-48对ABL野生型的IC50为1 nM，对ABL T315I突变体的IC50为0.8 nM。该化合物能够阻断BCR-ABL野生型与突变体的自磷酸化作用，并干扰下游的信号传导通路，如STAT5和CRKL，这进一步引发细胞周期的阻滞和细胞凋亡(Apoptosis)。此外，CHMFL-48有潜力作为研究慢性粒细胞白血病(CML)的工具。

Ladanein is a phytochemicals inhibitor that is known to disrupt the interactions of core and other hepatitis C virus (HCV) proteins.Ladanein possesses free radicals DPPH and ABTS +.scavenging activity, it also displays moderate (20-40 microM) activities against K562, K562R (imatinib-resistant), and 697 human leukemia cell lines.