Toceranib

SKU: orb1220006

Description

Toceranib phosphate is an orally active inhibitor of tyrosine kinase (RTK) receptor, and it potently inhibits PDGFR, VEGFR, and Kit(with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively), has antitumor and antiangiogenic activity.Administration of toceranib significantly decreased the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving toceranib and CYC demonstrated a significant increase in serum concentrations of IFN-γ, which was inversely correlated with Treg numbers after 6 weeks of combination treatment.

Images & Validation

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Key Properties

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CAS Number	356068-94-5
MW	396.46
Purity	>98% (HPLC)
Formula	C₂₂H₂₅FN₄O₂
SMILES	Cc1[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c(C)c1C(=O)NCCN1CCCC1
Target	PDGFR
Solubility	DMSO:2.4 mg/mL (6.05 mM; Need ultrasonic)

Bioactivity

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In Vivo

Administration of Toceranib significantly decreases the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving Toceranib 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.

In Vitro

Toceranib (SU11654) 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. 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 na ve, 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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SU11654,PHA 291639E

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PDGFR

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Toceranib (orb1220006)

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Purity:	97.62% (May vary between batches)
CAS Number:	356068-94-5
MW:	396.46
Formula:	C₂₂H₂₅FN₄O₂

Purity:	98.56% (May vary between batches)
CAS Number:	874819-74-6
MW:	494.45
Formula:	C₂₂H₂₈FN₄O₆P

Purity:	>98% (HPLC)
CAS Number:	874819-74-6
MW:	494.45
Formula:	C₂₂H₂₈FN₄O₆P

Toceranib

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Toceranib (orb1220006)

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