Alphabetical listing of all products

A - B - C - D - E - F - G - H - I - J - K - L - M - N - O - P - Q - R - S - T - U - V - W - X - Y - Z

Prices
  • 25 mg - 85 EUR
  • 100 mg - 255 EUR
  • 250 mg - 510 EUR

17-AAG

17-AAG (17-N-Allylamino-17-demethoxygeldanamycin) is a derivative of the antibiotic geldanamycin that is being tested in the treatment of cancer. 17-AAG exerts its effect by inhibiting the ATPase activity of the heat shock protein HSP90, resulting in degradation of HSP90 client proteins via the ubiquitin proteosome pathway.

catalogue number: A001
synonyms: Tanespimycin, NSC330507, CP 127374
CAS: 75747-14-7
MW: 585.69 g/mol

References
Future Oncol. 2005 Apr;1(2):273-81. PMID: 16555999
Curr Mol Med. 2009 Jun;9(5):654-64. PMID: 19601813

Prices
  • 5 mg - 195 EUR
  • 25 mg - 780 EUR
  • 100 mg - 2330 EUR

A-966492

A-966492 displayed high potency against the poly(ADP-ribose) polymerase-1 (PARP-1) enzyme with a K(i) of 1 nM and an EC(50) of 1 nM in a whole cell assay. In addition, it is orally bioavailable, crosses the blood-brain barrier, and appears to distribute into tumor tissue.

catalogue number: A004
synonyms: 22b
CAS: 934162-61-5
MW: 324.35 g/mol

References
J Med Chem. 2010 Apr 22;53(8):3142-53. PMID: 20337371

Prices
  • 5 mg - 148 EUR
  • 25 mg - 592 EUR
  • 100 mg - 1776 EUR

ABT-263

ABT-263 is a potent and orally bioavailable Bcl-2 family inhibitor. It disrupts interactions between Bcl-2/Bcl-xL and pro-death proteins (e.g., Bim), leading to the initiation of apoptosis. In human tumor cells, ABT-263 induces Bax translocation, cytochrome c release, and subsequent apoptosis.

catalogue number: A005
synonyms: Navitoclax
CAS: 923564-51-6
MW: 974.61 g/mol

References
Cancer Res. 2008 May 1;68(9):3421-8. PMID: 18451170

Prices
  • 5 mg - 148 EUR
  • 25 mg - 592 EUR
  • 100 mg - 1776 EUR

ABT-737

ABT-737 is a small-molecule inhibitor of protein-protein interactions that primarily affects the anti-apoptotic proteins Bcl-2, Bcl-X(L) and Bcl-w. Rather than directly initiating the apoptotic process, it enhances the effects of death signals, displaying synergistic cytotoxicity with chemotherapeutics and radiation. ABT-737 improves survival, causes regression of established tumours, and produces cures in a high percentage of tested mice.

catalogue number: A006
CAS: 852808-04-9
MW: 813.43 g/mol

References
Nature. 2005 Jun 2;435(7042):677-81. PMID: 15902208
Cell Death Differ. 2007 Sep;14(9):1711-3. PMID: 17572662
Crystal structure of Bcl-xL in complex with ABT-737 2YXJ

Prices
  • 5 mg - 74 EUR
  • 25 mg - 296 EUR
  • 100 mg - 888 EUR

ABT-888

ABT-888 is a potent inhibitor of both PARP-1 and PARP-2 with K(i)s of 5.2 and 2.9 nmol/L, respectively. The compound has good oral bioavailability and crosses the blood-brain barrier. ABT-888 strongly potentiated temozolomide in the B16F10 s.c. murine melanoma model.

catalogue number: A007
synonyms: Veliparib
CAS: 912444-00-9
MW: 244.29 g/mol

References
Clin Cancer Res. 2007 May 1;13(9):2728-37. PMID: 17473206
Crystal structure of PARP fragment with ABT-888 3KJD

Prices
  • 5 mg - 230 EUR
  • 25 mg - 920 EUR
  • 100 mg - 2760 EUR

AC220

Quizartinib (AC220) is a small molecule receptor tyrosine kinase inhibitor that is currently under development for the treatment of acute myeloid leukaemia. Its molecular target is FLT3, also known as CD135, against which it has an IC50 of 0.56 nM.

catalogue number: A008
synonyms: Quizartinib
CAS: 950769-58-1
MW: 560.67 g/mol

References
Blood. 2009 Oct 1;114(14):2984-92. PMID: 19654408
J Med Chem. 2009 Dec 10;52(23):7808-16. PMID: 19754199

Prices
  • 5 mg - 60 EUR
  • 25 mg - 240 EUR
  • 100 mg - 720 EUR

Adriamycin

Adriamycin is an anthracycline antibiotik that intercalates into DNA and causes DNA damage. It is commonly used in the treatment of a wide range of cancers, including hematological malignancies, many types of carcinoma, and soft tissue sarcomas. It inhibits the progression of the enzyme topoisomerase II by stabilizing the complex formed after the enzyme has broken the DNA chain during replication. This prevents the resealing of the double helix and thereby halts replication.

catalogue number: A009
synonyms: Doxorubicin, Rubex, NSC-123127
CAS: 25316-40-9
MW: 579.98 g/mol

References
Cancer Chemother Rep. 1969 Feb;53(1):33-7. PMID: 5772652
Biochimie. 1984 May;66(5):333-52. PMID: 6380596

Prices
  • 5 mg - 85 EUR
  • 25 mg - 340 EUR
  • 100 mg - 1020 EUR

Afatinib

Afatinib is a tyrosine kinase inhibitor that irreversibly inhibits the activity of human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. It is a candidate drug against non-small cell lung carcinoma, glioma, and cancers of the breast, prostate, head and neck.

catalogue number: A010
synonyms: BIBW2992
CAS: 850140-72-6
MW: 485.94 g/mol

References
Strahlenther Onkol. 2007 May;183(5):256-64. PMID: 17497097
Oncogene. 2008 Aug 7;27(34):4702-11. PMID: 18408761
Br J Cancer. 2011 Nov 8;105(10):1554-62. PMID: 21970876

Prices
  • 5 mg - 98 EUR
  • 25 mg - 392 EUR
  • 100 mg - 1176 EUR

Aminopurvalanol

Aminopurvalanol is a potent cyclin-dependent kinase inhibitor; it has IC50 values of 33 nM for Cdk1/cyclin B, 28 nM for Cdk2/cyclin E, and 20 nM for Cdk5/p35. Aminopurvalanol-treated cells acquired phenotypic characteristics of differentiated macrophages and underwent cell cycle with a 4N DNA content. Affinity chromatography and biochemical reconstitution experiments indicated that it targets cyclin-dependent kinase 1 (CDK1).

catalogue number: A011
synonyms:
CAS: 220792-57-4
MW: 403.91 g/mol

References
J Med Chem. 2006 Jun 29;49(13):3826-31. PMID: 10220373
X-ray structure of human CDK6-V cyclin with the inhibitor aminopurvalanol 2F2C

Prices
  • 5 mg - 165 EUR
  • 25 mg - 660 EUR
  • 100 mg - 1980 EUR

Apatinib mesylate

Apatinib is an orally bioavailable tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2/KDR) with IC50 value of 2.4 nM. Inhibition of this important pro-angiogenic receptor blocks VEGF-mediated endothelial cell migration and proliferation that in turn reduces new blood vessel formation in tumor tissue. It is being developed as a potential targeted treatment for metastatic gastric carcinoma, metastatic breast cancer and advanced hepatocellular carcinoma.

catalogue number: A111
synonyms: YN968D1
CAS: 1218779-75-9
MW: 493.58 g/mol (mesylate)

References
Cancer Res. 2010 Oct 15;70(20):7981-91. PMID: 20876799
Cancer Sci. 2011 Jul;102(7):1374-80. PMID: 21443688

Prices
  • 5 mg - 140 EUR
  • 25 mg - 560 EUR
  • 100 mg - 1680 EUR

AT7519

AT7519 is a potent inhibitor of several cyclin-dependent kinases (CDKs) that showed potent antiproliferative activity (40-940 nmol/L) in a panel of human tumor cell lines. Short-term treatments inhibited phosphorylation of the transcriptional marker RNA polymerase II and caused downregulation of the antiapoptotic protein Mcl-1, without affecting the abundance of XIAP or Bcl-2. The reduced abundance of the Mcl-1 protein level was linked to an increase in cleaved poly(ADP-ribose) polymerase. The mechanism of action was shown to be consistent with the inhibition of CDK1, CDK2 and CDK9 in tumor cell lines.

catalogue number: A012
CAS: 844442-38-2
MW: 382.24 g/mol

References
J Med Chem. 2008 Aug 28;51(16):4986-99. PMID: 18656911
Mol Cancer Ther. 2009 Feb;8(2):324-32. PMID: 19174555
Oncogene. 2010 Apr 22;29(16):2325-36. PMID: 20101221
PDB Structure of its co-crystal with CDK2: 2VTQ

Prices
  • 25 mg - 52 EUR
  • 100 mg - 156 EUR
  • 250 mg - 312 EUR

Axitinib

Axitinib is a potent and selective oral inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. It inhibits cellular autophosphorylation of VEGF receptors (VEGFR) with picomolar IC50 values. Counterscreening across multiple kinase and protein panels showed that it is selective for VEGFRs. Axitinib blocks VEGF-mediated endothelial cell survival, tube formation, and downstream signaling through endothelial nitric oxide synthase, Akt and extracellular signal-regulated kinase. It was approved for use in patients with renal cell carcinoma that had failed to respond to a previous treatment.

catalogue number: A013
synonyms: AG-013736, Inlyta
CAS: 319460-85-0
MW: 386.47 g/mol

References
Clin Cancer Res. 2008 Nov 15;14(22):7272-83. PMID: 19010843
Curr Oncol Rep. 2011 Apr;13(2):103-11. PMID:21318618

Prices
  • 25 mg - 22 EUR
  • 100 mg - 65 EUR
  • 250 mg - 130 EUR

5-azacytidine

5-azacytidine is an analogue of cytidine used in the treatment of myelodysplastic syndrome. It is a potent inhibitor of methyltransferases and its application reduces the level of DNA methylation. Its antineoplastic activity is partly due to this inhibition of DNA methylation and partly due to its incorporation into RNA, which disrupts RNA metabolism.

catalogue number: A113
synonyms: Azacitidine, Mylosar, Ladakamycin, Vidaza
CAS: 320-67-2
MW: 244.2 g/mol

References
Recent Results Cancer Res. 2010;184:159-70. PMID: 20072837

Prices
  • 5 mg - on request
  • 25 mg - on request
  • 100 mg - on request

Azathioprine

Azathioprine is an immunosuppressive purine analogue. The compound itself is a prodrug: following oral ingestion, it is metabolized into 6-mercaptopurine, which inhibits purine synthesis. 6-Mercaptopurine impedes DNA synthesis and thus inhibits cellular proliferation.

catalogue number: A114
synonyms: Azamun, Azasan, Imuran, BW-57-322, NSC-39084
CAS: 446-86-6
MW: 277.26 g/mol

References
J Clin Invest. 2003 Apr;111(8):1122-4. PMID: 12697731

Prices
  • 5 mg - 88 EUR
  • 25 mg - 352 EUR
  • 100 mg - 1056 EUR

AZD5438

AZD5438 is a potent inhibitor of cyclin-dependent kinases (CDKs) 1, 2, and 9 (IC50, 16, 6, and 20 nmol/L, respectively). It exhibits significant in vitro antiproliferative activity in human tumor cell lines (with IC(50) values ranging from 0.2-1.7 micromol/L), inhibiting the phosphorylation of CDK substrates including pRb, nucleolin, protein phosphatase 1a, and the carboxy-termiinal domain of RNA polymerase II. In this way, it blocks cell cycle progression in the G(2)-M, S, and G(1) phases. It is currently undergoing clinical trials as an anticancer drug.

catalogue number: A014
synonyms: -
CAS: 602306-29-6
MW: 371.46 g/mol

References
Mol Cancer Ther. 2009 Jul;8(7):1856-66. PMID: 19509270

Prices
  • 5 mg - 74 EUR
  • 25 mg - 296 EUR
  • 100 mg - 888 EUR

AZD8055

AZD8055 is a potent, selective, and orally bioavailable mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. It is an ATP-competitive inhibitor of mTOR kinase activity, with an IC50 of 0.8 nmol/L. AZD8055 showed excellent selectivity (approximately 1,000-fold) against all class I phosphatidylinositol 3-kinase (PI3K) isoforms and other members of the PI3K-like kinase family. Moreover, it exhibited no significant activity against a panel of 260 kinases at concentrations of up to 10 micromol/L. AZD8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as that of the mTORC2 substrate AKT and downstream proteins.

catalogue number: A015
synonyms: -
CAS: 1009298-09-2
MW: 465.54 g/mol

References
Cancer Res. 2010 Jan 1;70(1):288-98. PMID: 20028854