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219499 CEP-701 - CAS 111358-88-4 - Calbiochem

219499
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
111358-88-4C₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O
Description
Overview

This product has been discontinued.



A cell-permeable indolocarbazole that is reported to inhibit the activity of several tyrosine kinases, including JAK2/3, Flt3, TrkA, Flk1/KDR/VEGFR2, (IC50 = 0.9, 3, 3.4, and 65 nM, respectively, in cell-free kinase assays) and RET, while exhibiting much reduced potency against PKC and PDGFRβ (IC50 = 218 and 773 nM, respectively) and little or no effect towards EGFR, βIRK, FMS, KIT, or Bcr-Abl. CEP-701 is shown to exhibit anti-cancer efficacy in numerous cultures in vitro as well as in murine and rat xenograft models via subcutaneous or oral dosage (10 to 30 mg/kg, b.i.d.) in vivo.

Catalogue Number219499
Brand Family Calbiochem®
SynonymsKT-5555, VEGFR Tyrosine Kinase Inhibitor XXXIII, VEGFR2 Kinase Inhibitor XXXI, PDGFR Tyrosine Kinase Inhibitor XX, JAK2 Inhibitor VIII, JAK3 Inhibitor IX
References
ReferencesHexner, E.O., et al. 2008. Blood 111, 5663.
Strock, C.J., 2003. Cancer Res. 63, 5559.
Zheng, R., et al. 2002. Blood 100, 4154.
Levis, M., et al. 2002. Blood 99, 3885.
Miknyoczki, S.J., et al. 1999. Clin. Cancer Res. 5, 2205.
Miknyoczki, S.J., et al. 1999. Ann. N.Y. Acad. Sci. 880, 252.
George, D.J., et al. 1999. Cancer Res. 59, 2395.
Product Information
CAS number111358-88-4
FormOff-white solid
Hill FormulaC₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O
Chemical formulaC₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Regulatory Review
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
219499 0

Documentation

CEP-701 - CAS 111358-88-4 - Calbiochem Certificates of Analysis

TitleLot Number
219499

References

Reference overview
Hexner, E.O., et al. 2008. Blood 111, 5663.
Strock, C.J., 2003. Cancer Res. 63, 5559.
Zheng, R., et al. 2002. Blood 100, 4154.
Levis, M., et al. 2002. Blood 99, 3885.
Miknyoczki, S.J., et al. 1999. Clin. Cancer Res. 5, 2205.
Miknyoczki, S.J., et al. 1999. Ann. N.Y. Acad. Sci. 880, 252.
George, D.J., et al. 1999. Cancer Res. 59, 2395.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision15-July-2010 RFH
SynonymsKT-5555, VEGFR Tyrosine Kinase Inhibitor XXXIII, VEGFR2 Kinase Inhibitor XXXI, PDGFR Tyrosine Kinase Inhibitor XX, JAK2 Inhibitor VIII, JAK3 Inhibitor IX
DescriptionA cell-permeable indolocarbazole that is reported to inhibit the activity of several tyrosine kinases, including JAK2/3, Flt3, TrkA, Flk1/KDR/VEGFR2, (IC50 = 0.9, 3, 3.4, and 65 nM, respectively, in cell-free kinase assays) and RET, while exhibiting much reduced potency against PKC and PDGFRβ (IC50 = 218 and 773 nM, respectively) and little or no effect towards EGFR, βIRK, FMS, KIT, or Bcr-Abl. CEP-701 is shown to exhibit anti-cancer efficacy in numerous cultures in vitro as well as in murine and rat xenograft models via subcutaneous or oral dosage (10 to 30 mg/kg, b.i.d.) in vivo.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number111358-88-4
Chemical formulaC₂₆H₂₁N₃O₄ •0.5H₂O •0.5C₃H₈O
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml) or Ethanol (1 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Regulatory Review
ReferencesHexner, E.O., et al. 2008. Blood 111, 5663.
Strock, C.J., 2003. Cancer Res. 63, 5559.
Zheng, R., et al. 2002. Blood 100, 4154.
Levis, M., et al. 2002. Blood 99, 3885.
Miknyoczki, S.J., et al. 1999. Clin. Cancer Res. 5, 2205.
Miknyoczki, S.J., et al. 1999. Ann. N.Y. Acad. Sci. 880, 252.
George, D.J., et al. 1999. Cancer Res. 59, 2395.