Uzansertib(Synonyms: INCB053914)

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Uzansertib (Synonyms: INCB053914)

Uzansertib (INCB053914) 是一种具有口服活性的，ATP 竞争性泛-PIM 激酶抑制剂，对于 PIM1，PIM2 和 PIM3 的 IC50 分别为 0.24 nM，30 nM 和 0.12 nM。Uzansertib 对多种血液肿瘤细胞系具有广泛的抗增殖活性。

Uzansertib(Synonyms: INCB053914)

Uzansertib Chemical Structure

CAS No. : 1620012-39-6

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Uzansertib 的其他形式现货产品:

Uzansertib phosphate

生物活性

Uzansertib (INCB053914) 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 has broad anti-proliferative activity against a variety of hematologic tumor cell lines[1].

IC50 & Target[1]

PIM1

0.24 nM (IC50)

PIM2

30 nM (IC50)

PIM3

0.12 nM (IC50)

体外研究
(In Vitro)

Uzansertib 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[1].
Uzansertib (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[1].
PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib (mean IC50, 4 nM and 27 nM, respectively)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Uzansertib (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 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

513.51

Formula

C26H26F3N5O3
CAS 号

1620012-39-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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