
INCB053914 phosphate
CAS No. 2088852-47-3
INCB053914 phosphate( —— )
Catalog No. M23938 CAS No. 2088852-47-3
INCB053914 phosphate is an orally active, ATP-competitive inhibitor of pan-PIM kinase.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
5MG | 266 | In Stock |
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10MG | 397 | In Stock |
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25MG | 656 | In Stock |
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50MG | 888 | In Stock |
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100MG | 1251 | In Stock |
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200MG | Get Quote | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameINCB053914 phosphate
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NoteResearch use only, not for human use.
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Brief DescriptionINCB053914 phosphate is an orally active, ATP-competitive inhibitor of pan-PIM kinase.
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DescriptionINCB053914 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).(In Vitro):Uzansertib phosphate inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI50 values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines.Uzansertib phosphate (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines.PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib phosphate (mean IC50, 4 nM and 27 nM, respectively).(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) .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) .
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In VitroUzansertib phosphate inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI50 values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines. Uzansertib phosphate (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines. PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib phosphate (mean IC50, 4 nM and 27 nM, respectively).
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In VivoUzansertib 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) . 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) . Animal Model:Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)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.
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Synonyms——
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PathwayJAK/STAT Signaling
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TargetPim
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RecptorPIM1|PIM2|PIM3
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Research Area——
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Indication——
Chemical Information
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CAS Number2088852-47-3
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Formula Weight611.51
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Molecular FormulaC26H29F3N5O7P
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Purity>98% (HPLC)
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SolubilityDMSO: 5 mg/mL (8.18 mM; Need ultrasonic and warming)
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SMILESO=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
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Koblish H, et al. Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies. PLoS One. 2018 Jun 21;13(6):e0199108.
molnova catalog



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INCB053914 phosphate
INCB053914 phosphate is an orally active, ATP-competitive inhibitor of pan-PIM kinase.