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Src Inhibitor 1 (Src-I1) is a novel, potent and selective dual site inhibitor of Src tyrosine kinases with potential anticancer activity. It acts by competitively binding to both the ATP- and peptide-binding sites (IC50 = 44 nM for Src and 88nM for Lck, respectively). Src is a non-receptor tyrosine kinase that is deregulated in many types of cancer. Thus Src Inhibitor 1 (Src-I1) can be potentially used for cancer treatment.
| ln Vitro |
Src Inhibitor 1 competes with the ATP and peptide binding sites of the kinase. For both Src and Lck, the IC50 values of Src Inhibitor 1 are 44 and 88 nM, respectively[1]. Strong Src Inhibitor 1 (IC50=0.18 μM) was discovered to inhibit not only Src but also other members of the Src family, including Yes, Lck, and Csk, with potencies comparable to Src, and RIP2 (IC50=0.026 μM) showing greater efficacy. Moreover, Src Inhibitor 1's inhibitory potency on CHK2 is comparable to that of Src, while it is marginally less potent on Aurora B [2].
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| ln Vivo |
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| References |
[1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.
[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315 |
| Molecular Formula |
C22H19N3O3
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| Molecular Weight |
373.41
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| CAS # |
179248-59-0
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| Related CAS # |
Src I1; Src I-1; SrcI1.;
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| SMILES |
Chemical Name:6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine InChi Key:DMWVGXGXHPOEPT-UHFFFAOYSA-N InChi Code:InChI=1S/C22H19N3O3/c1-26-20-12-18-19(13-21(20)27-2)23-14-24-22(18)25-15-8-10-17(11-9-15)28-16-6-4-3-5-7-16/h3-14H,1-2H3,(H,23,24,25) SMILES:COC1=CC2=NC=NC(NC3=CC=C(OC4=CC=CC=C4)C=C3)=C2C=C1OC |
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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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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.91 mg/mL (2.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 9.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 0.91 mg/mL (2.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 9.1 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6780 mL | 13.3901 mL | 26.7802 mL | |
| 5 mM | 0.5356 mL | 2.6780 mL | 5.3560 mL | |
| 10 mM | 0.2678 mL | 1.3390 mL | 2.6780 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.
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