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Tyrosine kinase inhibitor
Tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Also shown to inhibit the transmembrane receptor kit and platelet-derived growth factor (PDGF) receptors.
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Product Details
| Alternative Name |
STI-571, CGP-57148B |
|---|---|
| Appearance |
White to pale yellow crystalline powder. |
| CAS |
220127-57-1 |
| Couple Target |
Abl, PDGF receptor |
| Couple Type |
Inhibitor |
| Formula |
C29H31N7O . CH3SO3H |
| MI |
14: 4902 |
| MW |
493.6 . 96.1 |
| Purity |
≥98% (HPLC) |
| Solubility |
Soluble in water (200mg/ml) or DMSO (100mg/ml) or DMF (10mg/ml) or PBS (2mg/ml). Sparingly soluble in ethanol (0.2mg/ml). Storing aqueous solutions for more than one day is not recommended. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Long Term Storage |
+4°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Distinct and targetable role of calcium-sensing receptor in leukaemia: R.S. Pereira, et al.; Nat. Commun. 14, s41467 (2023), Abstract
- An organ-on-chip model of pulmonary arterial hypertension identifies a BMPR2-SOX17-prostacyclin signalling axis: A.J. Ainscough, et al.; Commun. Biol. 5, 1192 (2022), Abstract
- Combination of PKCδ Inhibition with Conventional TKI Treatment to Target CML Models: F. Muselli, et al.; Cancers 13, 1693 (2021), Abstract — Full Text
- Targeting Discoidin Domain Receptors DDR1 and DDR2 overcomes matrix-mediated tumor cell adaptation and tolerance to BRAF-targeted therapy in melanoma: I. Berestjuk, et al.; EMBO Mol. Med. , e11814 (2021), Abstract
- A MICROFLUIDIC CHIP FOR PULMONARY ARTERIAL HYPERTENSION: Wojciak-Stothard, B., Ainscough, A., et al.; Research Square , (2021)
- Combined chemical genetics and data-driven bioinformatics approach identifies receptor tyrosine kinase inhibitors as host-directed antimicrobials: C.J. Korbee, et al.; Nat. Commun. 9, 358 (2018), Abstract — Full Text
- Direct modification of the 5-HT3 receptor current by some anticancer drugs: Y. Nakamura, et al.; Eur. J. Pharmacol. 821, 21 (2017), Abstract
- Importance of pulmonary vein preferential fibrosis for atrial fibrillation promotion in hypertensive rat hearts: Y. Iwasaki, et al.; Can. J. Cardiol. 32, 767 (2016), Application(s): Cell Culture, Abstract
- Identifying and validating a combined mRNA and microRNA signature in response to imatinib treatment in a chronic myeloid leukemia cell line: Bhutra, S., Lenkala, D., et al.; PLoS One 9, e115003 (2014), Abstract
- Imatinib treatment causes substantial transcriptional changes in adult Schistosoma mansoni in vitro exhibiting pleiotropic effects: C. Buro, et al.; PLoS Negl. Trop. Dis. 8, e2923 (2014), Application(s): Treatment of Xenopus oocytes and S. mansoni worms, Abstract — Full Text
- The role of γ-secretase activating protein (GSAP) and imatinib in the regulation of γ-secretase activity and amyloid-β generation: Hussain, I., Fabrègue, J., et al.; J. Biol. Chem. 288, 2521 (2013), Abstract
- The conformational control inhibitor of tyrosine kinases DCC-2036 is effective for imatinib-resistant cells expressing T674I FIP1L1-PDGFRα: Shen, Y., Shi, X., et al.; PLoS One 8, e73059 (2013), Abstract
- Salmonella modulation of host cell gene expression promotes its intracellular growth: Hannemann, S., Gao, B., et al.; PLoS Pathog. 9, e1003668 (2013), Abstract
- Quantification of kinase activity in cell lysates via photopatterned macroporous poly(ethylene glycol) hydrogel arrays in microfluidic channels: Lee, A. G., Beebe, D. J., et al.; Biomed. Microdevices 14, 247 (2012), Abstract
- Characterization of the Src/Abl hybrid kinase SmTK6 of Schistosoma mansoni: Beckmann, S., Hahnel, S., et al.; J. Biol. Chem. 286, 42325 (2011), Abstract
- Pristimerin induces apoptosis in imatinib-resistant chronic myelogenous leukemia cells harboring T315I mutation by blocking NF-kappaB signaling and depleting Bcr-Abl: Lu, Z., Jin, Y., et al.; Mol. Cancer 9, 112 (2010), Abstract
- Combination of imatinib and vinorelbine enhances cell growth inhibition in breast cancer cells via PDGFR beta signalling: M.T. Weigel, et al.; Cancer Lett. 273, 70 (2009), Abstract
- Imatinib as a novel therapeutic approach for fibrotic disorders: J.H. Distler & O. Distler; Rheumatology (Oxford) 48, 2 (2009), Abstract
- Is autophagy rather than apoptosis the regression driver in imatinib-treated gastrointestinal stromal tumors?: F. Miselli, et al.; Transl. Oncol. 1, 177 (2008), Abstract
- Imatinib mesylate for the treatment of chronic myeloid leukemia: S. Soverini, et al.; Expert Rev. Anticancer Ther. 8, 853 (2008), (Review), Abstract
- Imatinib: C.E. de Kogel & J.H. Schellens; Oncologist 12, 1390 (2007), (Review), Abstract
- The kinase inhibitor imatinib–an immunosuppressive drug?: D. Wolf, et al.; Cancer Drug Targets 7, 251 (2007), (Review), Abstract
- Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors: E. Buchdunger, et al.; J. Pharmacol. Exp. Ther. 295, 139 (2000), Abstract
- Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative: E. Buchdunger, et al.; Cancer Res. 56, 100 (1996), Abstract
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