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Uzansertib phosphate (INCB053914 phosphate) is an orally active, ATP-competitive inhibitor of pan-PIM kinase(PIM1, PIM2, PIM3 with IC50s of 0.24 nM, 30 nM, 0.12 nM , respectively).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $89 | In Stock | In Stock | |
| 5 mg | $228 | In Stock | In Stock | |
| 10 mg | $347 | In Stock | In Stock | |
| 25 mg | $625 | In Stock | In Stock | |
| 50 mg | $876 | - | In Stock | |
| 100 mg | $1,220 | - | In Stock |
| Description | Uzansertib phosphate (INCB053914 phosphate) is an orally active, ATP-competitive inhibitor of pan-PIM kinase(PIM1, PIM2, PIM3 with IC50s of 0.24 nM, 30 nM, 0.12 nM , respectively). |
| Targets&IC50 | Pim3:0.12 nM, Pim2:30 nM, Pim1:0.24 nM |
| In vitro | INCB053914, a novel, potent, and selective adenosine triphosphate-competitive pan-PIM kinase inhibitor.?In vitro, INCB053914 inhibited proliferation and the phosphorylation of downstream substrates in cell lines from multiple hematologic malignancies. |
| In vivo | Effects were confirmed in primary bone marrow blasts from patients with acute myeloid leukemia treated ex vivo and in blood samples from patients receiving INCB053914 in an ongoing phase 1 dose-escalation study.?In vivo, single-agent INCB053914 inhibited Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts.?Additive or synergistic inhibition of tumor growth was observed when INCB053914 was combined with selective PI3Kδ inhibition, selective JAK1 or JAK1/2 inhibition, or cytarabine. |
| Synonyms | INCB053914 phosphate |
| Molecular Weight | 611.51 |
| Formula | C26H29F3N5O7P |
| Cas No. | 2088852-47-3 |
| Smiles | O=C(C1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1)NC3=CN=C4C(CC[C@H]4O)=C3N5C[C@@H](N)[C@H](O)[C@@H](C)C5.O=P(O)(O)O |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (8.18 mM), Sonication and heating are recommended. | |||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.64 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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