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

Tandutinib

Tandutinib is a potent inhibitor of the FLT3, platelet-derived growth factor receptor (PDGFR), and c-Kit kinases (IC50 approximately 200 nM), but has little effect on other tyrosine or serine/threonine kinases. Tandutinib inhibited FLT3 phosphorylation, downstream signaling and malignant growth in vitro and in animal models. The compound displayed promising antileukemic activity (90% complete remissions) in a phase I/II trial in patients with newly diagnosed AML when administered in combination with cytarabine and daunorubicin. It is currently undergoing Phase II clinical trials in patients with AML or renal cell carcinoma.

catalogue number: T107
synonyms: MLN518, CT53518
CAS: 387867-13-2
MW: 562.72 g/mol

References
Cancer Cell. 2002 Jun;1(5):421-32. PMID: 12124172
J Med Chem. 2002 Aug 15;45(17):3772-93. PMID: 12166950
IDrugs. 2008 Jan;11(1):46-56. PMID: 18175263

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

Telatinib

Telatinib is an orally active small-molecule tyrosine kinase inhibitor that targets the kinase insert domain receptor (KDR; VEGFR-2) and the fms-related tyrosine kinase 4 (FLT4; VEGFR-3). Treatment with Telatinib inhibits angiogenesis and cellular proliferation in tumors in which these receptors are upregulated.

catalogue number: T112
synonyms: BAY 57-9352
CAS: 332012-40-5
MW: 409.83 g/mol

References
Invest New Drugs. 2011 Feb;29(1):137-43. PMID: 19924384

Prices
  • 5 mg - 56 EUR
  • 25 mg - 224 EUR
  • 100 mg - 672 EUR

Temsirolimus

Temsirolimus is a water-soluble synthetic rapamycin ester that has been developed for both oral and intravenous applications. Like rapamycin, temsirolimus is an inhibitor of the protein kinase mTOR, which is important for the synthesis of proteins that regulate proliferation and thus for cellular growth and survival. Inhibition of mTOR abrogates pathway-mediated cellular transcription and translation, leading to cell cycle arrest, antiangiogenesis and apoptosis. Temsirolimus has significant in vitro antitumor effects against a number of cancer cell lines and has demonstrated in vivo cytostatic activity in xenograft models. Patients receiving temsirolimus alone achieved longer survival than those receiving interferon alone or temsirolimus plus interferon in a randomized phase III trial. It has been approved as a drug for the treatment of renal cell carcinoma.

catalogue number: T076
synonyms: CCI-779, Torisel
CAS: 162635-04-3
MW: 1030.28 g/mol

References
Proc Natl Acad Sci U S A. 2001 Aug 28;98(18):10320-5. PMID: 11504907
Drugs Today (Barc). 2007 Oct;43(10):659-69. PMID: 17987219
Recent Results Cancer Res. 2010;184:189-97. PMID: 20072839

Prices
  • 5 mg - 280 EUR
  • 25 mg - 1120 EUR
  • 100 mg - 3360 EUR

TG02

TG02 is a novel pyrimidine-based multi-kinase inhibitor that inhibits CDKs 1, 2, 7 and 9 together with JAK2 and FLT3; IC50 values are 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively. TG02 is cytotoxic in a broad range of tumor cell lines, inducing G1 cell cycle arrest, both the intrinsic and extrinsic pathways of apoptosis, depletion of XIAP and the key multiple myeloma survival protein Mcl-1. It is currently undergoing clinical trials in advanced leukemias and multiple myeloma.

catalogue number: T169
synonyms: SB1317, SB-1317
CAS: 937270-47-8
MW: 372.47 g/mol

References
Leukemia. 2012 Feb;26(2):236-43. PMID: 21860433
J Med Chem. 2012 Jan 12;55(1):169-96. PMID: 22148278
Clin Cancer Res. 2013 Mar 26. [Epub ahead of print] PMID: 23532886

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

TG101348

TG101348 is a potent and selective ATP-competitive JAK2 inhibitor with an IC50 of 3 nM; it is active also towards the JAK2 V617F mutant. TG101348 also inhibits the Flt3 and Ret kinases with IC50 values of 15 and 48 nM, respectively. It exhibits significantly less activity against other tyrosine kinases, including JAK3 (IC50=169 nM). In treated cells, it blocks downstream cellular signalling (JAK-STAT), suppressing proliferation and inducing apoptosis. It is currently being developed for the treatment of patients with myeloproliferative diseases including myelofibrosis.

catalogue number: T110
synonyms: TG-101348, fedratinib
CAS: 936091-26-8
MW: 524.68 g/mol

References
Leukemia. 2008 Sep;22(9):1790-2. PMID: 18354492
Cancer Cell. 2008 Apr;13(4):311-20. PMID: 18394554

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

Thalidomide

Thalidomide is a potent inhibitor of new blood vessel growth (angiogenesis) and is effective against several types of cancers. It intercalates into DNA in guanine-cytosine-rich regions, which affects the promoter regions of the genes that control the development of limbs, ears, and eyes, such as IGF-I and FGF-2. The subsequent loss of immature blood vessels is the primary cause of thalidomide-induced teratogenesis and may also be the mechanism of its anti-angiogenic activity.

catalogue number: T129
synonyms: Thalomid
CAS: 50-35-1
MW: 258.23 g/mol

References
Proc Natl Acad Sci U S A. 2009 May 26;106(21):8573-8. PMID: 19433787

Prices
  • 5 mg - 238 EUR
  • 25 mg - 952 EUR
  • 100 mg - 2856 EUR

Tipifarnib

Tipifarnib is a potent and selective inhibitor of farnesyl protein transferase that has significant antitumor effects in vivo. Tipifarnib competitively inhibits the farnesylation of lamin B and K-RasB peptide substrates, with IC50 values of 0.86 nM and 7.9 nM, respectively. Tumor cell lines bearing H-ras or N-ras mutations were among the most sensitive of the cell lines tested, with responses observed at nanomolar concentrations of tipifarnib. The activity of this compound in the myeloid malignancies of myelodysplastic syndrome, myelofibrosis and elderly/high-risk acute myeloid leukemia is of particular interest.

catalogue number: T108
synonyms: Zarnestra, R115777
CAS: 192185-72-1
MW: 489.4 g/mol

References
Cancer Res. 2001 Jan 1;61(1):131-7. PMID: 11196150
Expert Rev Anticancer Ther. 2006 Mar;6(3):313-9. PMID: 16503848

Prices
  • 5 mg - 80 EUR
  • 25 mg - 320 EUR
  • 100 mg - 960 EUR

Tivozanib

Tivozanib is an orally active, ATP-competitive inhibitor of VEGFR tyrosine kinase developed for the potential treatment of cancer. Tivozanib inhibits activation of VEGFR-1, VEGFR-2 and VEGFR-3 at picomolar concentrations. In preclinical studies, tivozanib produced a significant inhibition of tumor growth and angiogenesis in several different animal models.

catalogue number: T146
synonyms: AV-951, KRN-951
CAS: 475108-18-0
MW: 454.86 g/mol

References
IDrugs. 2010 Sep;13(9):636-45. PMID: 20799147
Clin Cancer Res. 2011 Nov 15;1 PMID: 21976547

Prices
  • 25 mg - 110 EUR
  • 100 mg - 330 EUR
  • 250 mg - 660 EUR

Topotecan

Topotecan is an inhibitor of topoisomerase I used to treat ovarian, cervical and lung cancer. Treatment of cells with this compound inhibits DNA replication and transcription and activates DNA damage checkpoints.

catalogue number: T130
synonyms: Hycamtin, NSC 609699
CAS: 119413-54-6
MW: 457.91 g/mol (hydrochloride)

References
Nat Rev Cancer. 2006 Oct;6(10):789-802. PMID: 16990856

Tozasertib

See product V080 VX-680

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

Trametinib

Trametinib is a potent and selective allosteric inhibitor of the MEK1 and MEK2 kinases with strong antitumor activity. Trametinib inhibits prevents Raf-dependent MEK phosphorylation (S217 for MEK1), producing prolonged p-ERK1/2 inhibition. Cell growth inhibition is significant in most tumor lines with mutant BRAF or Ras. It undergoes trials in patients with metastatic BRAF-mutant melanoma.

catalogue number: T167
synonyms: GSK-1120212, JTP-74057
CAS: 871700-17-3
MW: 615.41 g/mol

References
Clin Cancer Res. 2011 Mar 1;17(5):989-1000. PMID: 21245089
J Clin Oncol. 2013 Feb 1;31(4):482-9. PMID: 23248257

Prices
  • 5 mg - 284 EUR
  • 25 mg - 1136 EUR
  • 100 mg - 3408 EUR

Trichostatin A

Trichostatin A is a specific inhibitor of the class I and II mammalian histone deacetylases (HDAC). It has been shown to cause the accumulation of acetylated histones with subsequent cell cycle arrest, terminal differentiation and/or apoptosis in various cancer cell lines, and to inhibit tumor growth in animals.

catalogue number: T077
synonyms: TSA
CAS: 58880-19-6
MW: 302.37 g/mol

References
J Biol Chem. 1990 Oct 5;265(28):17174-9. PMID: 2211619
J Biol Chem. 1993 Oct 25;268(30):22429-35. PMID: 8226751

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

Tyrphostin AG 490

Tyrphostin AG-490 potently inhibits the kinase activities of JAK2 and JAK3. Inhibition of Jak-2 activity by AG-490 selectively blocks leukaemic cell growth in vitro and in vivo by inducing programmed cell death (acute lymphoblastic leukaemia), with no deleterious effect on normal haematopoiesis. AG490 also suppresses cell proliferation and induces apoptosis in IL-6-dependent multiple myeloma cell lines. AG-490 inhibits JAK3-dependent activation of STAT5a/b and downstream signal transduction and cellular proliferation of antigen-activated human T cells.

catalogue number: T150
synonyms: Tyrphostin B42
CAS: 134036-52-5
MW: 294.30 g/mol

References
Nature. 1996 Feb 15;379(6566):645-8. PMID: 8628398

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

Tyrphostin AG 1478

Tyrphostin AG 1478 is a specific inhibitor of the EGF-receptor tyrosine kinase (ERBB1) activity with an IC50 of about 3 nM in vitro. It is also very active against L858R and L861Q EGFR mutants. According to Invitrogen profiling, it displays moderate activity also against ERBB2 (HER2) and ERBB4 (HER4) receptors, LYNA and LYNB. AG1478 has very weak activity on PDGF and HER2-NEU kinases (IC50 values over 100 microM).

catalogue number: T151
synonyms: AG 1478
CAS: 175178-82-2
MW: 315.75 g/mol

References
Eur J Biochem. 1994 Nov 1;225(3):1047-53. PMID: 7525285
J Leukoc Biol. 1999 Jun;65(6):891-9. PMID: 10380915
Br J Haematol. 2000 Jun;109(4):823-8. PMID: 10929036