化学性质
| Storage | Store at -20°C |
| M.Wt | 524.47 |
| Cas No. | 854001-07-3 |
| Formula | C22H27Cl2N7O2S |
| Synonyms | BMS-354825 hydrochloride;Sprycel hydrochloride;BMS354825 hydrochloride;BMS 354825 hydrochloride |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥8.41 mg/mL in DMSO with ultrasonic |
| Chemical Name | (Z)-N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carbimidic acid hydrochloride |
| Canonical SMILES | CC1=C(/N=C(O)/C(S2)=CN=C2NC3=CC(N4CCN(CCO)CC4)=NC(C)=N3)C(Cl)=CC=C1.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
资料参考
Description:
IC50 Value: 0.6 nM (Abl); 0.8 nM (Src) [1]
Dasatinib is an oral multi- BCR/Abl and Src family tyrosine kinase inhibitor approved for first line use in patients with chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia(Ph+ ALL).
in vitro: Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range. Dasatinib directly targets wild-type and mutant Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Dasatinib displays 325-fold greater potency compared with imatinib against cells expressing wild-type Bcr-Abl [1]. DSB and radiotherapy induced a significant growth delay in both HNSCC xenograft models, although to a lesser extent in SCCNij202. DSB did not inhibit phosphorylated protein kinase B (pAKT) or phosphorylated extracellular signal-regulated kinase 1/2 (pERK1/2) but did inhibit (phosphorylated) DNA-dependent protein kinase [2].
in vivo: Daily oral administration of dasatinib delays tumour onset and increases overall survival but does not inhibit the proliferation of established tumours. The striking difference between the dasatinib-treated group of tumours and the vehicle controls was the prominent squamous metaplasia that was seen in six out of 11 dasatinib-treated tumours [3]. In vivo studies were performed in a nude mouse xenograft model, the new prescription (DDP + Dasatinib) was better than DDP alone in terms of therapeutic efficacy [4].
Toxicity: Major cytogenetic response was significantly (P < 0.01) associated with weighted average steady-state dasatinib plasma concentrations, and pleural effusion was significantly associated with trough concentration [5]. We present a patient with chronic myelogenous leukemia who developed nephrotic-range proteinuria after initiation ondasatinib therapy that resolved after changing therapy to imatinib [6].
Clinical trial: Dasatinib, Cytarabine, and Idarubicin in Treating Patients With High-Risk Acute Myeloid Leukemia. Phase 1/Phase 2
