dasatinib

Dasatinib (BMS-354825) 是一种酪氨酸激酶抑制剂，抑制 Src 和 Bcr-Abl (Ki=16 30 pM)，具有口服活性和 ATP 竞争性。Dasatinib 具有抗肿瘤活性，用于治疗白血病和淋巴瘤等。

Dasatinib monohydrate (BMS-354825 Monohydrate) 是一种具有口服活性的，ATP 竞争性的双重Src Bcr-Abl 抑制剂，有抗肿瘤活性，还诱导凋亡和自噬。它抑制Src 和Bcr-Abl 的IC50分别为 0.5 nM 和 <1.0 nM，Ki 值分别为 16 pM 和 30 pM。

Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) 基于 ABL 抑制剂达沙替尼，通过接头与 IAP 配体结合，形成 SNIPER [1]。

Dasatinib Analog-1，其Ki值为5.4 μM，能够抑制CYP3A4活力，并能阻断谷胱甘肽加合物的形成。

Dasatinib D8 is deuterium-labeled dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

Dasatinib metabolite M6 (Dasatinib carboxylic acid) is an oxidative metabolite of Dasatinib, a potent and orally active inhibitor of both Bcr-Abl and Src family tyrosine kinases[1].

N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) 是 Dasatinib 的代谢物，是以达沙替尼为基础的分子，通过连接体与 IAP 配体结合，形成 SNIPER，从而降解 ABL。N-Deshydroxyethyl Dasatinib 可用于研究癌症和免疫疾病。

Dasatinib hydrochloride (BMS-354825 HCl) (BMS-354825) hydrochloride 是一种具有口服活性的，ATP 竞争性的，双重 Src Bcr-Abl 抑制剂，具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 Ki 值分别为 16 pM 和 30 pM。Dasatinib hydrochloride hydrochloride 抑制 Bcr-Abl 和 Src 的IC50 分别为 <1.0 nM 和 0.5 nM。Dasatinib hydrochloride hydrochloride 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。

Hydroxymethyl dasatinib (M24), a benzylhydroxy metabolite of Dasatinib, demonstrates potent activity with an IC50 value of 46.7 nM in K562 CML cells [1].

Dasatinib N-oxide 是 Dasatinib 的一种次要代谢物。Dasatinib 是口服有效的Src Bcr-Abl 抑制剂。

BMS-748730, also known as 4′-Hydroxy Dasatinib, is a Dasatinib metabolite.

Antitumor photosensitizer-4 (compound 10b) 是靶向ABCG2酪氨酸激酶抑制剂(TKI)的有效代表，由达沙替尼与伊马替尼构成的光敏剂(PS)。该化合物能够诱发细胞凋亡(apoptosis)及ROS生成，在HepG2和B16-F10细胞上展现出显著的光毒性作用。

SJ11646是一种高效的LCK（淋巴细胞特异性蛋白酪氨酸激酶）降解剂（PROTAC；DC50= 0.00838 pM）。该化合物由Dasatinib作为LCK配体，以及基于苯基谷氨酰亚胺的cereblon结合体组成。它在体外对LCK激活的T细胞急性淋巴细胞白血病（T-ALL）细胞株和初级白血病样本展现出细胞毒性。在体内，SJ11646在源自患者的T-ALL异种移植模型中显示出抗白血病效果。

APcK110 is a novel Kit inhibitor . APcK110 inhibits proliferation of the mastocytosis cell line HMC1.2 and the SCF-responsive cell line OCI/AML3 in a dose-dependent manner . APcK110 is a more potent inhibitor of OCI/AML3 proliferation than the clinically used Kit inhibitors imatinib and dasatinib and at least as potent as cytarabine. APcK110 inhibits the phosphorylation of Kit, Stat3, Stat5, and Akt in a dose-dependent fashion, showing activity of APcK110 on Kit and its downstream signaling pathways . APcK110 may have potent application in AML.

SNIPER(ABL)-020 is a chemical compound consisting of Dasatinib, an ABL inhibitor, and Bestatin, an IAP ligand, conjugated with a linker. This compound effectively reduces the BCR-ABL protein[1].

SGX393 is an inhibitor of the CML mutant Bcr-AblT315I, thereby preempting in vitro resistance when combined with nilotinib or dasatinib.

SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively[1].

SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM[1].