PD 082106

PD 082106 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; IC₅₀ = 0.015 µM, respectively) and a derivative of indirubin (Item No. 14155).¹ It is selective for FLT3 over Met, Ron, EGFR, and the insulin receptor (IC₅₀s = >10 µM for all) but does inhibit DRAK2 (IC₅₀ = 0.62 µM), as well as VEGFR2 and Aurora A (IC₅₀s = 1.53 and 1.27 µM, respectively).^1,2 PD 082106 inhibits proliferation of A549 lung, SNU-638 stomach, HT-1080 fibrosarcoma, HL-60 leukemia, and MCF-7 breast cancer cells with IC₅₀ values of 13, 2.1, 3.4, 89, and 9 µM, respectively, but does not inhibit proliferation of Col 2 colon cancer cells.³ It also inhibits proliferation of (IC₅₀ = 5.1 µM), and induces apoptosis in, K-Ras-transformed RK3D rat kidney epithelial (RK3E-ras) cells and reduces tumor growth in RK3E-ras flank and oral tumor models.⁴ PD 082106 is active against the parasite T. gondii (ID₅₀ = 0.52 µM) with a toxic dose value (TD₅₀) of 61 µM.⁵

WARNING This product is not for human or veterinary use.

1. Choi, S.-J., Lee, J.-E., Jeong, S.-Y., et al. 5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. J. Med. Chem. 53(9), 3696-3706 (2010).

2. Jung, M.E., Byun, B.J., Kim, H.-M., et al. Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening. Bioorg. Med. Chem. Lett. 26(11), 2719-2723 (2016).

3. Moon, M.J., Lee, S.K., Lee, J.-W., et al. Synthesis and structure-activity relationships of novel indirubin derivatives as potent anti-proliferative agents with CDK2 inhibitory activities. Bioorg. Med. Chem. 14(1), 237-246 (2006).

4. Kim, S.-A., Kim, Y.-C., Kim, S.-W., et al. Antitumor activity of novel indirubin derivatives in rat tumor model. Clin. Cancer Res. 13(1), 253-259 (2007).

5. Krivogorsky, B., Grundt, P., Yolken, R., et al. Inhibition of Toxoplasma gondii by indirubin and tryptanthrin analogs. Antimicrob. Agents Chemother. 52(12), 4466-4469 (2008).