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Prices
  • 5 mg - 75 EUR
  • 25 mg - 300 EUR
  • 100 mg - 900 EUR

GDC-0449

GDC-0449 is a small, orally available inhibitor of the Hedgehog (Hh) pathway, which is involved in tumorigenesis. This provides a strong rationale for its use in the treatment of various cancers. The compound suppresses Hh signaling by binding to and interfering with smoothened (with an IC50 of 3 nM), a membrane protein that provides positive signals to the Hh signaling pathway. Vismodegib is currently undergoing phase II clinical trials for the treatment of advanced BCC, metastatic colorectal cancer, ovarian cancer, MB and other solid tumors. Because of its low toxicity and specificity for the Hh pathway, this drug has potential advantages over conventional chemotherapeutic agents and could potentially be useful in combination treatments.

catalogue number: G033
synonyms: Vismodegib, Erivedge
CAS: 879085-55-9
MW: 421.3 g/mol

References
Curr Opin Investig Drugs. 2010 Jun;11(6):707-18. PMID: 20496266

Prices
  • 5 mg - 52 EUR
  • 25 mg - 208 EUR
  • 100 mg - 624 EUR

Gefitinib

Gefitinib is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase domain, which is sometimes referred to as Her1 or ErbB-1. Gefitinib blocks signal transduction pathways implicated in the proliferation and survival of cancer cells and other host-dependent processes that promote cancer growth.

catalogue number: G034
synonyms: Iressa, ZD-1839
CAS: 184475-35-2
MW: 446.9 g/mol

References
Drugs. 2000;60 Suppl 1:33-40 PMID: 11129170
www.iressa.com

Prices
  • 5 mg - 194 EUR
  • 25 mg - 776 EUR
  • 100 mg - 2328 EUR

Geldanamycin

Geldanamycin is a benzoquinone ansamycin antibiotic that binds to and inhibits the functioning of heat shock protein 90 (Hsp90). Despite its potent antitumor potential, geldanamycin presents several major drawbacks as a drug candidate. This has stimulated the development of geldanamycin analogues, and especially analogues bearing modifications at the 17 position such as 17-AAG and 17-DMAG.

catalogue number: G035
synonyms:
CAS: 30562-34-6
MW: 560.64 g/mol

References
Proc Natl Acad Sci U S A. 1994 Aug 30;91(18):8324-8. PMID: 8078881
Cancer Lett. 2010 Apr 1;290(1):24-35. PMID: 19850405

Prices
  • 25 mg - 103EUR
  • 100 mg - 309 EUR
  • 250 mg - 618 EUR

Genistein

Genistein is an isoflavone-related natural product. It influences multiple biochemical pathways in cells, including those involved in PPAR activation, the activation of estrogen receptors, and topoisomerase activity. In addition, it displays direct antioxidative activity. The molecular mechanism of its anticancer activity is probably related to its ability to inhibit several tyrosine kinases.

catalogue number: G036
synonyms: AXP-CT-001
CAS: 446-72-0
MW: 270.24 g/mol

References
Cancer Lett. 2008 Oct 8;269(2):226-42. PMID: 18492603

Prices
  • 5 mg - 550 EUR
  • 25 mg - 2200 EUR

Gö 6976

Gö 6976 inhibits the Ca(2+)-dependent isozymespf protein kinase C (PKC) alpha and beta 1 at nanomolar concentrations. Kinetic analysis revealed that PKC inhibition by Gö 6976 is competitive with respect to ATP, non-competitive with respect to the protein substrate, and mixed type with respect to phosphatidylserine.

catalogue number: G140
synonyms: PD 406976, Go 6976
CAS: 136194-77-9
MW: 378.43 g/mol

References
J Biol Chem. 1993 May 5;268(13):9194-7. PMID: 8486620
Proc Natl Acad Sci U S A. 1993 May 15;90(10):4674-8. PMID: 7685108

Prices
  • 5 mg - 305 EUR
  • 25 mg - 1220 EUR
  • 100 mg - on request

GSK1210151A

GSK1210151A is an inhibitor of BET family of acetyl-lysine recognizing, chromatin proteins. The mode of action of GSK1210151A is based on the inhibition of transcription through the displacement of BRD3/4, PAFc and SEC components from chromatin. GSK1210151A has profound efficacy against human and murine mixed lineage leukaemia (MLL-fusions) and has also a potential for the treatment of inflammations.

catalogue number: G164
synonyms: I-BET151
CAS: 1300031-49-5
MW: 415.44 g/mol

References
Nature. 2011 Oct 2;478(7370):529-33. PMID: 21964340
Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. PMID: 22437115
PDB Structure of its co-crystal with human BRD4: PDB: 3ZYU

Prices
  • 25 mg - 72 EUR
  • 100 mg - 216 EUR
  • 250 mg - 432 EUR

GW2580

GW2580 is an orally bioavailable inhibitor of cFMS receptor kinase. It completely inhibited human cFMS kinase in vitro at 0.06 microM. GW2580 selectively inhibited cFMS kinase compared with 186 other kinases in vitro and completely inhibited CSF-1-induced growth of rat monocytes, with an IC50 value of 0.2 microM. GW2580 at 1 microM completely inhibited CSF-1-induced growth of mouse myeloid cells and human monocytes and completely inhibited bone degradation in cultures of human osteoclasts, rat calvaria, and rat fetal long bone.

catalogue number: G141
synonyms: -
CAS: 870483-87-7
MW: 366.41 g/mol

References
Proc Natl Acad Sci U S A. 2005 Nov 1;102(44):16078-83. PMID: 16249345
J Pharmacol Exp Ther. 2008 Jul;326(1):41-50. PMID: 18434589