Uzansertib phosphate(Synonyms: INCB053914 phosphate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Uzansertib phosphate (Synonyms: INCB053914 phosphate) 纯度: 98.44%

Uzansertib (INCB053914) phosphate 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 phosphate 对多种血液肿瘤细胞系具有广泛的抗增殖活性。

Uzansertib phosphate(Synonyms: INCB053914 phosphate)

Uzansertib phosphate Chemical Structure

CAS No. : 2088852-47-3

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1 mg ¥1200 In-stock
5 mg ¥3600 In-stock
10 mg ¥5400 In-stock
25 mg ¥9800 In-stock
50 mg ¥15000 In-stock
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生物活性

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].

IC50 & Target[1]

PIM1

0.24 nM (IC50)

PIM2

30 nM (IC50)

PIM3

0.12 nM (IC50)

体外研究
(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[1].
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[1].
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)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

上海金畔生物科技有限公司 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.

Clinical Trial

分子量

611.51

Formula

C26H29F3N5O7P

CAS 号

2088852-47-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 5 mg/mL (8.18 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6353 mL 8.1765 mL 16.3530 mL
5 mM 0.3271 mL 1.6353 mL 3.2706 mL
10 mM

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

    此方案可获得 ≥ 1.8 mg/mL (2.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

    此方案可获得 ≥ 1.8 mg/mL (2.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

    此方案可获得 ≥ 1.8 mg/mL (2.94 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Uzansertib(Synonyms: INCB053914)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

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

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务