| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 1g |
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Purity: ≥98%
Toceranib phosphate (formerly known as PHA291639; SU11654), phosphate salt of Toceranib, is a novel and potent receptor tyrosine kinase (RTK) inhibitor with antineoplastic/anticancer activities. It inhibits PDGFRβ and Flk-1/KDR at 5 nM and 6 nM, respectively. It is an authorized veterinary medication used to treat canine mast cell tumors in dogs. Toceranib may also have an anti-angiogenic effect, but its main mechanism of action is probably inhibition of kit tyrosine kinase.
| Targets |
PDGFRβ (Ki = 5 nM); Flk-1 (Ki = 6 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
For PDGFR and Flk-1/KDR, two members of the split kinase RTK family, toceranib (SU11654) selectively inhibits tyrosine kinase activity at 5 and 6 nM, respectively.
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| Cell Assay |
The parental cell line is the canine C2 mastocytoma c-kit mutant cell line, which was obtained from spontaneously occurring cutaneous mast cell tumors (MCTs). In an incubator set at 37°C with 5% CO2 humidity and supplemented with 2 mM L-glutamine, 10% FBS, 100 g/mL Streptomycin, and 100 U/mL Penicillin, cells are grown in RPMI 1640 medium. C2 cells are grown in Toceranib concentrations ranging from 0.02 uM to 0.3 uM and increasing in increments of 0.025-0.05 uM to select C2 cells that are resistant to the drug. Over the course of seven months, three separate sublines that are resistant to toceranib are established[2].
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| Animal Protocol |
Dogs: We utilize fifteen dogs owned by clients who have advanced tumors. Toceranib 2.75 mg/kg is given to dogs once every other day. An oral cyclophosphamide (CYC) dose of 15 mg/m2 per day is added after two weeks. During the eight-week study period, flow cytometry is used to measure the number of Treg and lymphocyte subsets in blood. ELISA is utilized to quantify the levels of IFN-γ in serum.
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| References |
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| Molecular Formula |
C22H28FN4O6P
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| Molecular Weight |
494.46
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| Exact Mass |
494.17304979
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| Elemental Analysis |
C, 53.44; H, 5.71; F, 3.84; N, 11.33; O, 19.41; P, 6.26
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| CAS # |
874819-74-6
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| Related CAS # |
Toceranib;356068-94-5
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| Appearance |
Solid powder
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| SMILES |
CC1=C(NC(=C1C(=O)NCCN2CCCC2)C)/C=C\3/C4=C(C=CC(=C4)F)NC3=O.OP(=O)(O)O
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| InChi Key |
OORBROPMMRREB-HBPAQXCTSA-N
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| InChi Code |
InChI=1S/C22H25FN4O2.H3O4P/c1-13-19(12-17-16-11-15(23)5-6-18(16)26-21(17)28)25-14(2)20(13)22(29)24-7-10-27-8-3-4-9-27;1-5(2,3)4/h5-6,11-12,25H,3-4,7-10H2,1-2H3,(H,24,29)(H,26,28);(H3,1,2,3,4)/b17-12-;
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| Chemical Name |
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-(2-pyrrolidin-1-ylethyl)-1H-pyrrole-3-carboxamide;phosphoric acid
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| Synonyms |
SU-11654 phosphate; PHA291639 phosphate; SU 11654; PHA-291639 phosphate; SU11654; PHA 291639; Toceranib phosphate; Trade name: Palladia.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0224 mL | 10.1120 mL | 20.2241 mL | |
| 5 mM | 0.4045 mL | 2.0224 mL | 4.0448 mL | |
| 10 mM | 0.2022 mL | 1.0112 mL | 2.0224 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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