Toceranib Phosphate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Toceranib 磷酸盐是分裂激酶 RTK 家族多个成员（包括 Flk-1/KDR、PDGFR）酪氨酸激酶活性的选择性抑制剂。

Toceranib phosphate is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family including Flk-1/KDR PDGFR.

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.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.

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.

PHA 291639 phosphate | SU11654 phosphate

Others

Other Targets

Protein-tyrosine kinase 2

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874819-74-6

494.45

C22H28FN4O6P

>98% (HPLC)

DMSO:2.46 mg/mL (4.98 mM)

OP(O)(O)=O.Cc1[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c(C)c1C(=O)NCCN1CCCC1

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(-20℃)

With Ice Pack

≥ 2 years