Dasatinib hydrochloride - CAS 854001-07-3
Catalog number: 854001-07-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Dasatinib hydrochloride is a potent and dual Abl/ Src inhibitor. It inhibits c-Kit (WT)/c-Kit (D816V).
BMS-354825 hydrochloride; Sprycel hydrochloride
Canonical SMILES:
1.The use of betaine HCl to enhance dasatinib absorption in healthy volunteers with rabeprazole-induced hypochlorhydria.
Yago MR1, Frymoyer A, Benet LZ, Smelick GS, Frassetto LA, Ding X, Dean B, Salphati L, Budha N, Jin JY, Dresser MJ, Ware JA. AAPS J. 2014 Nov;16(6):1358-65. doi: 10.1208/s12248-014-9673-9. Epub 2014 Oct 2.
Many orally administered, small-molecule, targeted anticancer drugs, such as dasatinib, exhibit pH-dependent solubility and reduced drug exposure when given with acid-reducing agents. We previously demonstrated that betaine hydrochloride (BHCl) can transiently re-acidify gastric pH in healthy volunteers with drug-induced hypochlorhydria. In this randomized, single-dose, three-way crossover study, healthy volunteers received dasatinib (100 mg) alone, after pretreatment with rabeprazole, and with 1500 mg BHCl after rabeprazole pretreatment, to determine if BHCl can enhance dasatinib absorption in hypochlorhydric conditions. Rabeprazole (20 mg b.i.d.) significantly reduced dasatinib Cmax and AUC0-∞ by 92 and 78%, respectively. However, coadministration of BHCl significantly increased dasatinib Cmax and AUC0-∞ by 15- and 6.7-fold, restoring them to 105 and 121%, respectively, of the control (dasatinib alone). Therefore, BHCl reversed the impact of hypochlorhydria on dasatinib drug exposure and may be an effective strategy to mitigate potential drug-drug interactions for drugs that exhibit pH-dependent solubility and are administered orally under hypochlorhydric conditions.
2.Autophagy protects against dasatinib-induced hepatotoxicity via p38 signaling.
Yang X1, Wang J1, Dai J1, Shao J1, Ma J2, Chen C2, Ma S3, He Q1, Luo P1, Yang B1. Oncotarget. 2015 Mar 20;6(8):6203-17.
Liver dysfunction is a common side effect associated with the treatment of dasatinib and its mechanism is poorly understood. Autophagy has been thought to be a potent survival or death factor for liver dysfunction, which may shed the light on a novel strategy for the intervention of hepatotoxicity caused by dasatinib. In this study, we show for the first time that autophagy is induced, which is consistent with the formation of liver damage. Autophagy inhibition exacerbated dasatinib-induced liver failure, suggesting that autophagy acted as a self-defense mechanism to promote survival. Oxidative stress has been shown to be an important stimulus for autophagy and hepatotoxicity. Interestingly, dasatinib increased the activity of p38, which is a critical modulator of the oxidative stress related to liver injury and autophagy. p38 silencing significantly blocked LC3-II induction and p62 reduction by dasatinib, which was accompanied by increased caspase-3 and PARP cleavage, indicating that autophagy alleviated dasatinib-induced hepatotoxicity via p38 signaling.
3.A phase I/II study combining erlotinib and dasatinib for non-small cell lung cancer.
Gold KA1, Lee JJ1, Harun N2, Tang X1, Price J1, Kawedia JD1, Tran HT1, Erasmus JJ1, Blumenschein GR1, William WN1, Wistuba II1, Johnson FM3. Oncologist. 2014 Oct;19(10):1040-1. doi: 10.1634/theoncologist.2014-0228. Epub 2014 Aug 28.
BACKGROUND: EGFR and Src are frequently activated in non-small cell lung cancer (NSCLC). In preclinical models, combining EGFR and Src inhibition has additive synergistic effects. We conducted a phase I/II trial of the combination of Src inhibitor dasatinib with EGFR inhibitor erlotinib to determine the maximum tolerated dose (MTD), pharmacokinetic drug interactions, biomarkers, and efficacy in NSCLC.
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CAS 854001-07-3 Dasatinib hydrochloride

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