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PIM inhibitor 1 (phosphate)

Product Name
PIM inhibitor 1 (phosphate)
CAS No.
2088852-47-3
Chemical Name
PIM inhibitor 1 (phosphate)
Synonyms
CS-2873;INCB053914 phosphate;INCB053914（Uzansertib）;Uzansertib (phosphate);PIM inhibitor 1 (phosphate);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;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
CBNumber
CB23309539
Molecular Formula
C26H29F3N5O7P
Formula Weight
611.51
MOL File
2088852-47-3.mol
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PIM inhibitor 1 (phosphate) Property

storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-6903
Product name
INCB053914(phosphate)
Purity
99.91%
Packaging
1mg
Price
$180
Updated
2021/12/16
ChemScene
Product number
CS-6903
Product name
INCB053914(phosphate)
Purity
99.91%
Packaging
25mg
Price
$1560
Updated
2021/12/16
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PIM inhibitor 1 (phosphate) Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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PIM inhibitor 1 (phosphate) Suppliers

China 38 United States 4 USA 1 Global 43
Sichuan Wei Keqi Biological Technology Co., Ltd.
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028-81700200 18116577057
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028-81705658
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3003855609@qq.com
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
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+86-21-52996696
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Shanghai Send Pharmaceutical Technology Co., Ltd.
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50266790 18317173152
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QQ3382968513
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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010-50973130 18101056239
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Chuzhou KeMail Chemical Technology Co., Ltd
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0550-5196001 15000891977
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Zhejiang J&C Biological Technology Co.,Limited
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+1-2135480471 +1-2135480471;
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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marketing@targetmol.com
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InvivoChem
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Changzhou Chenhong Biotechnology Co., Ltd.
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+86-0519-85788828 +86-13775037613
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sales@chemrenpharm.com
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China
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2088852-47-3, PIM inhibitor 1 (phosphate)Related Search:


  • 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）
  • 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
  • Uzansertib (INCB053914) ，S8800
  • 2088852-47-3