KB SRC 4Potent and selective c-Src inhibitor CAS# 1380088-03-8 |
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| Cas No. | 1380088-03-8 | SDF | Download SDF |
| PubChem ID | 73349077 | Appearance | Powder |
| Formula | C32H23ClN8 | M.Wt | 555.03 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 20 mM in DMSO | ||
| Chemical Name | 3-(4-chlorophenyl)-1-[3-[3-[(3-phenylphenyl)methyl]triazol-4-yl]phenyl]pyrazolo[3,4-d]pyrimidin-4-amine | ||
| SMILES | C1=CC=C(C=C1)C2=CC(=CC=C2)CN3C(=CN=N3)C4=CC(=CC=C4)N5C6=C(C(=N5)C7=CC=C(C=C7)Cl)C(=NC=N6)N | ||
| Standard InChIKey | UHIZYQVRKSWIFO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C32H23ClN8/c33-26-14-12-23(13-15-26)30-29-31(34)35-20-36-32(29)41(38-30)27-11-5-10-25(17-27)28-18-37-39-40(28)19-21-6-4-9-24(16-21)22-7-2-1-3-8-22/h1-18,20H,19H2,(H2,34,35,36) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent and selective c-Src inhibitor (Ki = 44 nM); does not inhibit c-Abl at concentrations up to 125 μM. Selective between Src family members (Kd values are 86, 160, 240, 720, 3200, 4400, and >40,000 nM for c-Src, Lck, Fgr, Yes, Lyn, Hck and Fyn respectively). Significantly inhibits cell growth in 4T1 mammary carcinoma tumor cells. |
KB SRC 4 Dilution Calculator
KB SRC 4 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8017 mL | 9.0085 mL | 18.017 mL | 36.0341 mL | 45.0426 mL |
| 5 mM | 0.3603 mL | 1.8017 mL | 3.6034 mL | 7.2068 mL | 9.0085 mL |
| 10 mM | 0.1802 mL | 0.9009 mL | 1.8017 mL | 3.6034 mL | 4.5043 mL |
| 50 mM | 0.036 mL | 0.1802 mL | 0.3603 mL | 0.7207 mL | 0.9009 mL |
| 100 mM | 0.018 mL | 0.0901 mL | 0.1802 mL | 0.3603 mL | 0.4504 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Development of a highly selective c-Src kinase inhibitor.[Pubmed:22594480]
ACS Chem Biol. 2012 Aug 17;7(8):1393-8.
Generating highly selective probes to interrogate protein kinase function in biological studies remains a challenge, and new strategies are required. Herein, we describe the development of the first highly selective and cell-permeable inhibitor of c-Src, a key signaling kinase in cancer. Our strategy involves extension of traditional inhibitor design by appending functionality proposed to interact with the phosphate-binding loop of c-Src. Using our selective inhibitor, we demonstrate that selective inhibition is significantly more efficacious than pan-kinase inhibition in slowing the growth of cancer cells. We also show that inhibition of c-Abl kinase, an off-target of most c-Src inhibitors, promotes oncogenic cell growth.
KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
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