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Cellagen Technology
FLT3 inhibitor
AC220 (Quizartinib) is an orally-available, imidazobenzothiazole-based inhibitor of Flt3, with an in vitro Kd of 2 nM. In vitro cell studies show that AC220 has a IC50 of 0.5 nM for MV-411 cells. [1] In a variety of leukemic cell lines, AC220 inhibited Flt3 phosphorylation of MV4-11, MOLM-14, SEM-K2, and RS4-11 at IC50s of 1, 2, 4, and 4 nM, respectively. Furthermore, inhibition of cell proliferation on these same lines were measured as 0.3, 0.1, 0.4, and >10000 nM, respectively. [2]
In a KinomeScan panel of 402 kinases, AC220 has a high degree of specificity toward Flt3 with only mild inhibition of closely related RTKs such as KIT, PDGFR, RET, VEGFR2. [3]
Ina Flt3-ITD acute myeloid leukemia mouse model, AC220 was shown to extend significantly the survival at 1 mg/kg QD dosing, and eradicates tumors in a Flt3-dependent mouse xenograft model at 10 mg/kg. [3]
Cellagen Technology
FLT3 inhibitor
AC220 (Quizartinib) is an orally-available, imidazobenzothiazole-based inhibitor of Flt3, with an in vitro Kd of 2 nM. In vitro cell studies show that AC220 has a IC50 of 0.5 nM for MV-411 cells. [1] In a variety of leukemic cell lines, AC220 inhibited Flt3 phosphorylation of MV4-11, MOLM-14, SEM-K2, and RS4-11 at IC50s of 1, 2, 4, and 4 nM, respectively. Furthermore, inhibition of cell proliferation on these same lines were measured as 0.3, 0.1, 0.4, and >10000 nM, respectively. [2]
In a KinomeScan panel of 402 kinases, AC220 has a high degree of specificity toward Flt3 with only mild inhibition of closely related RTKs such as KIT, PDGFR, RET, VEGFR2. [3]
Ina Flt3-ITD acute myeloid leukemia mouse model, AC220 was shown to extend significantly the survival at 1 mg/kg QD dosing, and eradicates tumors in a Flt3-dependent mouse xenograft model at 10 mg/kg. [3]
