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Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells.
| Molecular Weight | 501.07 |
| Formula | C29H33ClN6 |
| CAS Number | 2294874-49-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 125 mg/mL (ultrasonic) |
| Storage | 4°C, protect from light |
| Related FLT3 Products |
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| Quizartinib (AC220)
Quizartinib (AC220) is a uniquely potent and selective FLT3 inhibitor. |
| KW-2449
KW-2449 is a novel multitargeted kinase inhibitor of FLT3, ABL and Aurora kinase with IC50 values of 6.6 nM, 14 nM and 48 nM. |
| Tandutinib
Tandutinib (MLN518, CT53518) is an orally active multitargeted tyrosine kinase inhibitor of FLT3 (IC50 = 0.22 μM), and it also inhibits c-Kit and PDGFR with IC50 values of 0.17 μM and 0.20 μM, respectively. Tandutinib has the ability to cross the blood-brain barrier. |
| FF-10101
FF-10101 is a novel irreversible FLT3 inhibitor. |
| TCS 359
TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM. |
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