Imatinib-STI571-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEImatinibCat. No.: HY-15463CAS No.: 152459-95-5Synonyms: STI571; CGP-57148B分式: CHNO分量: 493.6作靶點: c-Kit; Bcr-Abl; PDGFR; Autophagy作通路: Protein Tyrosine Kinase/RTK; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 month

2、s-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 40 mg/mL (81.04 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.0259 mL 10.1297 mL 20.2593 mL5 mM 0.4052 mL 2.0259 mL 4.0519 mL10 mM 0.2026 mL 1.0130 mL 2.0259 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Imat

3、inib (STI571)種酪氨酸激酶抑制劑，可抑制 c-Kit，Bcr-Abl 和 PDGFR。IC50 & Target PDGFR c-Kit100 nM (IC50) 100 nM (IC50)體外研究Imatinib (STI571) inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEtotal protein levels of c-kit, MAP

4、K, or Akt. The concentration that produces 50% inhibition for these effects isapproximately 100 nM 1. Imatinib (STI571) is very effective (in vitro IC50 of 25 nM) against the chronicmyeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC50, 410 nM) andPDGFR (in v

5、itro IC50, 380 nM) 2. Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and inhibitsBcr/Abl, v-Abl, Tel/Abl, the native PDGF receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylati

6、on and cellgrowth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFR, and Tel/Arg with an IC50 of approximately0.5 M in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cellstransformed by Tel/JAK2 3. The IC50s of Imatinib(STI571) is a multi-target inhibito

7、r of v-Abl, c-Kit and onBON-1 and H727 cells after exposure for 48 h are 32.4 and 32.8 M, respectively 4.體內研究 In the phosphorothioate antisense oligodeoxynucleotides (PS-ASODN) group, tumor growth is inhibited by59.437%, which is markedly higher than in the Imatinib (STI571) is a multi-target inhibi

8、tor of v-Abl, c-Kit andgroup (11.071%) and liposome negative control group (2.759%). Telomerase activity is significantly lower (P5. Imatinib (25 mg/kg/day, p.o.) suppresses the growth of endometriotic tissue and reduces the number ofovarian follicles in a rat model. Imatinib effectively treats expe

9、rimental endometriosis by its inhibitor effects onangiogenesis and cell proliferation 6.PROTOCOLCell Assay 4 BON-1 cells (7,500 per well) and NCI-H727 cells (5,000 per well) are seeded into flat-bottomed 96-well platesin triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplement

10、ed DMEM or RPMI 1640complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) orserum-free medium containing serial dilutions of Imatinib. After 48 h (control cultures do not reachconfluence), the number of metabolically active cells is determined by the 3-

11、(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at540 nm. Growth inhibition is calculated. Experiments are done in triplicates 4.MCE has not independently confirmed the accuracy of these methods. They are for referen

12、ce only.Animal Mice 5Administration 56 The 40 tumor-bearing SCID mice are randomly divided into four groups (10 mice per group): the PS-ASODNgroup (5 M, each mouse receives 0.2 mL by intratumor injection once daily); Imatinib group (0.1 mg/g bodyweight); liposome negative control group (0.01 mL/g);

13、and saline group (0.01 mL/g). The mice in each groupreceive the relevant treatment by intra-tumor injection once daily from day 7 to day 28 after implantation.After 28 d, the mice are sacrificed, and tumor weight and longest and shortest diameters are measured byelectronic scale and vernier caliper,

14、 respectively. Inhibition of tumor growth is calculated.Rats 6Adult female Wistar-Albino rats (220-240 g) are used. Twenty-one days after the first surgical procedure, therats undergo a second laparotomy to evaluate the occurrence of endometriosis. Twenty-four rats havevisually confirmed endometriot

15、ic implants and are randomized into three groups to receive Imatinib (25mg/kg/day, p.o.), Anastrozole (0.004 mg/day, p.o.), or normal saline (0.1 mL, i.p.) for 14 days.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師

16、www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. Cancer Lett. 2019 Apr 10;447:105-114. Sci Signal. 2019 Jul 16;12(590). pii: eaav7259. J Med Chem. 2019 Jun.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1.

17、Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug1;96(3):925-32.2. Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin CancerRes.

18、 2007 Jun 1;13(11):3363-9.3. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-84. Yao JC, et al. Clinical and in vitro studies of imatinib in advanced carcinoid tumors. Clin Cancer Res. 2007 Jan 1;13(1):234-40.5. Sun XC, et al. Depletion of telomerase RNA inhibits growth of gastrointestinal tumors transplanted in mice. World J Gastroenterol. 2013Apr 21;19(15):2340-7.6. Yildiz C, et al. Effect of imatinib on growth of experimen