1. Protein Tyrosine Kinase/RTK
  2. PDGFR
  3. Toceranib phosphate

Toceranib phosphate (Synonyms: SU11654 phosphate; PHA 291639E phosphate)

目录号: HY-10330A 纯度: 98.02%

Toceranib phosphate (SU11654 phosphate) 是一种具有口服活性的酪氨酸激酶 (RTK) 受体抑制剂,能有效抑制 PDGFRVEGFRKit,抑制 PDGFRβ 和 Flk-1/KDR 的 Ki 值分别为 5 nM 和 6 nM。Toceranib phosphate 具有抗肿瘤和抗血管生成活性,可用于犬肥大细胞肿瘤的研究。

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Toceranib phosphate Chemical Structure

Toceranib phosphate Chemical Structure

CAS No. : 874819-74-6

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Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors[1] [2].

IC50 & Target


5 nM (Ki)


6 nM (Ki)

(In Vitro)

Toceranib phosphate (PHA 291639 phosphate) is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including PDGFR and Flk-1/KDR, with Kis of 5 and 6 nM, respectively[1].
To explore mechanisms of acquired Toceranib (TOC) resistance in canine MCT, three resistant sublines are generated from the Toceranib-sensitive exon 11 ITD c-kit mutant C2 cell line designated TR1, TR2, and TR3. Growth of the parental C2 cells is inhibited by Toceranib in a dose-dependent manner with an IC50 of <10 nM. In contrast, TR1, TR2, and TR3 sublines are resistant to inhibition by Toceranib (IC50> 1,000 nM). Sensitivity to three other KIT RTK inhibitors is similar to the observed resistance to Toceranib. The parental line as well as all three sublines retains sensitivity to the cytotoxic agents vinblastine (VBL) and CCNU. Following 72 hr culture in the presence of increasing concentrations of Toceranib, treatment naïve, parental C2 cells detach from the culture flask and become rounded, shrunken, and clumped with increased exposure to Toceranib. In contrast, Toceranib-induced morphologic differences are not identified in the resistant sublines[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

(In Vivo)

Administration of Toceranib phosphate (PHA 291639 phosphate) significantly decreases the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving Toceranib phosphate (PHA 291639 phosphate) and cyclophosphamide (CYC) demonstrate a significant increase in serum concentrations of IFN-γ, which is inversely correlated with Treg numbers after 6 weeks of combination treatment[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.








Room temperature in continental US; may vary elsewhere.


4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

In Vitro: 

DMSO : 2.46 mg/mL (4.98 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0224 mL 10.1122 mL 20.2245 mL
5 mM --- --- ---
10 mM --- --- ---

储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

Cell Assay

The c-kit mutant canine C2 mastocytoma cell line, derived from a spontaneously occurring cutaneous mast cell tumors (MCTs), is used as the parental cell line. Cells are propagated in RPMI 1640 supplemented with 2 mM L-glutamine, 10% FBS, 100 g/mL Streptomycin, and 100 U/mL Penicillin in a 37°C incubator under a humidified atmosphere of 5% CO2. Toceranib-resistant C2 cells are selected by growing C2 cells in concentrations of Toceranib ranging from 0.02 uM to 0.3 uM and increasing in 0.025-0.05 uM increments. Three independent, Toceranib -resistant sublines are established over a period of 7 months[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Fifteen client-owned dogs with advanced tumors are used. Dogs receive Toceranib at 2.75 mg/kg once every other day. After 2 weeks, oral cyclophosphamide (CYC) is added at 15 mg/m2 daily. Numbers of Treg and lymphocyte subsets are measured in blood by flow cytometry during the 8-week study period. Serum concentrations of IFN-γ are measured by ELISA.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2


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