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V-9077 Vargatef, Free Base, >99%       Prices Reduced (January 2012)

[BIBF1120] [Intedanib] [Nintedanib]

M.W. 539.62

C31H33N5O4

[928326-83-4]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 25 mg/mL with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Vargatef is an indolinone derivative that potently inhibits vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR) and fibroblast growth factor receptor (FGFR) kinase activity in enzymatic assays (table 1).  It blocks mitogen-activated protein kinase and Akt signaling pathways in three cell types contributing to angiogenesis, namely endothelial cells, pericytes, and smooth muscle cells, and it inhibits cell proliferation with an EC50 of 10-80 nM.  Hilberg, F., et al.  "BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy."  Cancer Res. 68:  4774-4782 (2008).

  Table 1. In vitro kinase inhibition profile of vargatef
  (adapted from Hilberg, F., et al. 2008).

  Kinase	IC50 (nM)*
  VEGFR-2 (mouse)	13 ± 4
  VEGFR-3	13 ± 10
  Lck	16 ± 16
  VEGFR-2	21 ± 13
  Flt-3	26
  VEGFR-1	34 ± 15
  FGFR-2	37 ± 2
  PDGFRα	59 ± 71
  PDGFRβ	65 ± 7
  FGFR-1	69 ± 70
  FGFR-3	108 ± 41
  Src	156 ± 40
  Lyn	195 ± 12
  FGFR-4	610 ± 117
  IGF1R	>1,000
  InsR	>4,000
  CDK1	>10,000
  CDK2	>10,000
  CDK4	>10,000
  Other kinases (n = 26)	>10,000
  EGFR	>50,000
  HER2	>50,000

  * Assays performed with ATP concentrations at the respective Ki.  Human kinases were tested except when stated otherwise.  Phosphatase PP2A and another 25 kinases were analyzed at 10 µM with 100 µM ATP:  GSK3B, ROCKII, DYRK1A, PKCα, MAPK2ERK2, HGFR, MSK1, PDK1, CHK1, MAPKAPK2, SAPK2AP38, S6K1, SGK, CK1, CK2, PKA, SAPK2BP38B2, SAPK3P38G, JNK1A1, SAPK4P38D, PHK, PKBA, CSK, CDK2/CYCLINA, PRAK (data not shown).

• Vargatef significantly decreased blood vessel area and inhibited tumour growth.  Zips, D., et al.  "Triple angiokinase inhibition, tumour hypoxia and radiation response of FaDu human squamous cell carcinomas."  Radiother. Oncol.  Apr 29 (2009) [Epub ahead of print].

• A reproducible hepatic perfusion index (HPI) was determined by using quantified gadopentetate dimeglumine (Gd-DTPA) concentration.  The HPI decreased significantly at 28 days after treatment with vargatef.  HPI may be useful for monitoring antiangiogenic treatment response of hepatic metastases.  Miyazaki, K., et al.  "Quantitative mapping of hepatic perfusion index using MR imaging: a potential reproducible tool for assessing tumour response to treatment with the antiangiogenic compound BIBF 1120, a potent triple angiokinase inhibitor."  Eur. Radiol. 18:  1414-1421 (2008).

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.