TSU-68 (Orantinib, SU6668)

Catalog No.: A10953

PDFGRβ inhibitor

TSU-68 (Orantinib, SU6668)

TSU-68 (Orantinib, SU6668) Chemical Structure

CAS NO. 252916-29-3

Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.

Availability: In stock

Package Price Qty
5 mg
$50.00
10 mg
$90.00
50 mg
$350.00
100 mg
$460.00
10mM * 1mL in DMSO
$90.00
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  • Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079

Biological Activity

Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
Targets
PDGFRβ (Cell-free assay) FGFR1 (Cell-free assay) Flk1 (Cell-free assay)
8 nM(Ki)1.2 μM(Ki)2.1 μM(Ki)
In vitro (25°C) DMSO 55 mg/mL (177.22 mM)
Water Insoluble
Ethanol Insoluble
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 28 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 32.22 mL 161.08 mL 322.16 mL
0.5 mM 6.44 mL 32.22 mL 64.43 mL
1 mM 3.22 mL 16.11 mL 32.22 mL
5 mM 0.64 mL 3.22 mL 6.44 mL

*The above data is based on the productmolecular weight 310.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A10953
Actions Inhibitor
CAS No. 252916-29-3
Formula C18H18N2O3
M. Wt 310.4
Purity >98%
Synonyms TSU68
SMILES CC1=C(NC(=C1CCC(=O)O)C)/C=C\2/C3=CC=CC=C3NC2=O
Storage

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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