An Hsp90 inhibitor
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HSP-990

Item No. 19149

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(7R)-2-amino-7-[4-fluoro-2-(6-methoxy-2-pyridinyl)phenyl]-7,8-dihydro-4-methyl-pyrido[4,3-d]pyrimidin-5(6H)-one
CAS Number
934343-74-5
Synonyms
  • NVP-HSP990
Molecular Formula
C20H18FN5O2
Formula Weight
379.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 25 mg/ml
λmax
269 nm
SMILES
COC1=NC(C2=C([C@@H]3NC(C(C(C)=NC(N)=N4)=C4C3)=O)C=CC(F)=C2)=CC=C1
InChi Code
InChI=1S/C20H18FN5O2/c1-10-18-16(26-20(22)23-10)9-15(25-19(18)27)12-7-6-11(21)8-13(12)14-4-3-5-17(24-14)28-2/h3-8,15H,9H2,1-2H3,(H,25,27)(H2,22,23,26)/t15-/m1/s1
InChi Key
WSMQUUGTQYPVPD-OAHLLOKOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    HSP-990 is an Hsp90 inhibitor with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and GRP94, respectively.1 It inhibits the TRAP1 ATPase with an IC50 value of 320 nM and demonstrates IC50 values of >5 µM in a panel of 51 unrelated kinases.1 In c-Met amplified GTL-16 gastric tumor cells, HSP-990 has been shown to dissociate the Hsp90-p23 complex, depleting the client protein c-Met and inducing Hsp70.1 HSP-990 can inhibit proliferation of various human tumor cell lines with GI50 values of 4-40 nM.1 Single oral administration of 15 mg/kg of HSP-990 was shown to induce sustained downregulation of c-Met and upregulation of Hsp70 in a GTL-16 xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Menezes, D.L., Taverna, P., Jensen, M.R., et al. The novel oral Hsp90 inhibitor NVP-HSP990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo. Mol. Cancer Ther. 11(3), 730-739 (2012).