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PIM inhibitor 1 (phosphate) manufacturers
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| | PIM inhibitor 1 (phosphate) Basic information |
| Product Name: | PIM inhibitor 1 (phosphate) | | Synonyms: | CS-2873;INCB053914 phosphate;PIM inhibitor 1 (phosphate);Uzansertib (phosphate);cell,inhibit,malignancies,INCB 053914,INCB-053914,Inhibitor,orally,Pim,INCB053914,ATP-competitive,tumor,Pim kinases,Uzansertib,hematologic,lines,broad,activity,anti-proliferative,Uzansertib phosphate;INCB053914（Uzansertib）;Uzansertib (INCB053914) ，S8800;N-((R)-4-((3R,4R,5S)-3-Amino-4-hydroxy-5-methylpiperidin-1-yl)-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide phosphate | | CAS: | 2088852-47-3 | | MF: | C26H29F3N5O7P | | MW: | 611.51 | | EINECS: | | | Product Categories: | | | Mol File: | 2088852-47-3.mol |  |
| | PIM inhibitor 1 (phosphate) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Solid | | color | White to off-white |
| | PIM inhibitor 1 (phosphate) Usage And Synthesis |
| Description | PAK4-IN-1 is an inhibitor of Pim extracted from patent WO 2017044730 A1, compound 1; has an IC50 of less than 35 nM. | | Uses | Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines[1]. | | in vivo | Uzansertib phosphate (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) [1].
Uzansertib phosphate demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC50=70 nM; KMS-12-BM tumors, IC50=145 nM) [1].
| Animal Model: | Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)[1] | | Dosage: | 25, 50, 75, 100 mg/kg | | Administration: | PO; twice a day; for 15 days | | Result: | Inhibited tumor growth in a dose-dependent manner in mice. |
| | IC 50 | PIM1: 0.24 nM (IC50); PIM2: 30 nM (IC50); PIM3: 0.12 nM (IC50) | | References | [1]. WO 2017044730 A1 |
| | PIM inhibitor 1 (phosphate) Preparation Products And Raw materials |
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