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Purity: ≥98%
SU 6656 (SU-6656) is a novel, potent and selective Src family kinase (Src, Yes, Lyn, and Fyn) inhibitor with potential antineoplastic activity. It inhibits Src, Yes, Lyn, and Fyn with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM respectively. SU6656 modulates CTGF (connective tissue growth factor) expression in an ERK-dependent manner. SU6656 induces caspase-independent cell death in FRO anaplastic thyroid carcinoma cells and therapeutic synergy in human synovial sarcoma growth, invasion and angiogenesis in vivo. In NIH 3T3 cell, SU6656 inhibits PDGF-/Src-driven mitogenesis and PDGF-stimulated c-Myc induction.
| ln Vitro |
In HNSCC cells, SU6656 lowers the phosphorylation of Src family kinase (SFK) [2].
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| ln Vivo |
Fall time increase caused by ischemia postconditioning (IPoCo) is greatly reduced by SU6656 (2-4 mg/kg; i.p.; once) [5].
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| Animal Protocol |
Animal/Disease Models: Swiss albino male mice[5]
Doses: 2, 4 mg/kg Route of Administration: intraperitoneal (ip)injection; once Experimental Results: Dramatically diminished IPoCo mediated increase in fall down time. |
| References |
[1]. Blake RA, et al. SU6656, a selective src family kinase inhibitor, used to probe growth factor signaling. Mol Cell Biol. 2000 Dec;20(23):9018-27.
[2]. Veracini L, et al. Elevated Src family kinase activity stabilizes E-cadherin-based junctions and collective movement of head and neck squamous cell carcinomas. Oncotarget. 2014 Dec 26. [3]. Wu ML, et al. Divergent signaling pathways cooperatively regulate TGFβ induction of cysteine-rich protein 2 in vascular smooth muscle cells. Cell Commun Signal. 2014 Mar 28;12:22. [4]. Ondrusová L, et al. Inhibition of mTORC1 by SU6656, the selective Src kinase inhibitor, is not accompanied by activation of Akt/PKB signalling in melanoma cells. Folia Biol (Praha). 2013;59(4):162-7. [5]. Kumar A, et al. Pharmacological investigations on possible role of Src kinases in neuroprotective mechanism of ischemic postconditioning in mice. Int J Neurosci. 2014 Oct;124(10):777-86. [6]. Liu XF, et al. Antitumor effects of immunotoxins are enhanced by lowering HCK or treatment with SRC kinase inhibitors. Mol Cancer Ther. 2014 Jan;13(1):82-9. |
| Molecular Formula |
C19H21N3O3S
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| Molecular Weight |
371.45
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| CAS # |
330161-87-0
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| Related CAS # |
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| SMILES |
O=S(C1=CC2=C(NC(/C2=C\C(N3)=CC4=C3CCCC4)=O)C=C1)(N(C)C)=O
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| InChi Key |
LOGJQOUIVKBFGH-YBEGLDIGSA-N
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| InChi Code |
InChI=1S/C19H21N3O3S/c1-22(2)26(24,25)14-7-8-18-15(11-14)16(19(23)21-18)10-13-9-12-5-3-4-6-17(12)20-13/h7-11,20H,3-6H2,1-2H3,(H,21,23)/b16-10-
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| Chemical Name |
(Z)-N,N-dimethyl-2-oxo-3-((4,5,6,7-tetrahydro-1H-indol-2-yl)methylene)indoline-5-sulfonamide
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| Synonyms |
SU 6656; SU-6656; SU6656;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6922 mL | 13.4608 mL | 26.9215 mL | |
| 5 mM | 0.5384 mL | 2.6922 mL | 5.3843 mL | |
| 10 mM | 0.2692 mL | 1.3461 mL | 2.6922 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effect of SU6656 on tyrosine phosphorylation.Mol Cell Biol.2000 Dec;20(23):9018-27. |
SU6656 inhibits PDGF-stimulated c-Myc induction.Mol Cell Biol.2000 Dec;20(23):9018-27. |
Effects of PP2, SU6656, and SU6657.
Inhibition of PDGF-stimulated NIH 3T3 cell DNA synthesis.Mol Cell Biol.2000 Dec;20(23):9018-27. |
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