| Identification | Back Directory | [Name]
PIM inhibitor 1 (phosphate) | [CAS]
2088852-47-3 | [Synonyms]
CS-2873
INCB053914 phosphate
Uzansertib (phosphate)
PIM inhibitor 1 (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 | [Molecular Formula]
C26H29F3N5O7P | [MDL Number]
MFCD31382184 | [MOL File]
2088852-47-3.mol | [Molecular Weight]
611.51 |
| Hazard Information | Back Directory | [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) | [storage]
Store at -20°C | [References]
[1]. WO 2017044730 A1 |
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| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
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