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Description: Potent and selective c-Src inhibitor
Chemical Name: 1-[3-[1-([1,1'-Biphenyl]-3-ylmethyl)-1H-1,2,3-triazol-5-yl]phenyl]-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Purity: ≥98% (HPLC)
Citations (4)

Biological Activity for KB SRC 4

KB SRC 4 is a 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.

Compound Libraries for KB SRC 4

KB SRC 4 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for KB SRC 4

M. Wt 555.03
Formula C32H23ClN8
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1380088-03-8
PubChem ID 73349077
Smiles NC1=C2C(N(C4=CC=CC(C5=CN=NN5CC6=CC(C7=CC=CC=C7)=CC=C6)=C4)N=C2C3=CC=C(Cl)C=C3)=NC=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for KB SRC 4

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 11.1 20

Preparing Stock Solutions for KB SRC 4

The following data is based on the product molecular weight 555.03. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 9.01 mL 45.04 mL 90.09 mL
1 mM 1.8 mL 9.01 mL 18.02 mL
2 mM 0.9 mL 4.5 mL 9.01 mL
10 mM 0.18 mL 0.9 mL 1.8 mL

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References for KB SRC 4

References are publications that support the biological activity of the product.

Brandvold et al (2012) Development of a highly selective c-Src kinase inhibitor. ACS Chem.Biol. 7 1393 PMID: 22594480

If you know of a relevant reference for KB SRC 4, please let us know.

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Keywords: KB SRC 4, KB SRC 4 supplier, KBSRC4, c-Src, Src, kinases, inhibitors, inhibits, 4T1, mammary, carcinoma, tumor, cells, breast, cancer, non-receptor, tyrosine, Kinases, 4660, Tocris Bioscience

4 Citations for KB SRC 4

Citations are publications that use Tocris products. Selected citations for KB SRC 4 include:

Dominique et al (2021) Biological characterization of ligands targeting the human CC chemokine receptor 8 (CCR8) reveals the biased signaling properties of small molecule agonists. Biochem Pharmacol 188 114565 PMID: 33872569

Kim et al (2014) An endoplasmic reticulum stress-initiated sphingolipid metabolite, ceramide-1-phosphate, regulates epithelial innate immunity by stimulating β-defensin production. Mol Cell Biol 34 4368 PMID: 25312644

Carmona et al (2016) Lamellipodin promotes invasive 3D cancer cell migration via regulated interactions with Ena/VASP and SCAR/WAVE. Oncogene 35 5155 PMID: 26996666

Joseph R et al (2020) The NMDAR modulator NYX-2925 alleviates neuropathic pain via a Src-dependent mechanism in the mPFC. Neurobiol Pain 7 100039 PMID: 31909296

Do you know of a great paper that uses KB SRC 4 from Tocris? Please let us know.

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