Uzansertib phosphate (Synonyms: INCB053914 phosphate)

Name: Uzansertib phosphate
Brand: MedChemExpress
SKU: HY-101870B
Rating: 4.5 (1 reviews)

Cat. No.: HY-101870B Purity: 99.39%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Uzansertib phosphate Chemical Structure

CAS No. : 2088852-47-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 377	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 377	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 756	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1058	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1480	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Uzansertib phosphate:

Uzansertib Get quote

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Pim Isoform Specific Products:

View All Isoforms

PIM1 PIM2 PIM3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PIM1

0.24 nM (IC₅₀)

PIM2

30 nM (IC₅₀)

PIM3

0.12 nM (IC₅₀)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) 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

Molecular Weight

611.51

Formula

C₂₆H₂₉F₃N₅O₇P

CAS No.

2088852-47-3

Appearance

Solid

Color

White to off-white

SMILES

O=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.OP(O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 18 mg/mL (29.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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	0.1635 mL	0.8176 mL	1.6353 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

This protocol yields a clear solution of ≥ 1.8 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

This protocol yields a clear solution of ≥ 1.8 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

This protocol yields a clear solution of ≥ 1.8 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.39%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (257 KB) HNMR (284 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6353 mL	8.1765 mL	16.3530 mL	40.8824 mL
	5 mM	0.3271 mL	1.6353 mL	3.2706 mL	8.1765 mL
	10 mM	0.1635 mL	0.8176 mL	1.6353 mL	4.0882 mL
	15 mM	0.1090 mL	0.5451 mL	1.0902 mL	2.7255 mL
	20 mM	0.0818 mL	0.4088 mL	0.8176 mL	2.0441 mL
	25 mM	0.0654 mL	0.3271 mL	0.6541 mL	1.6353 mL

Uzansertib phosphate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Uzansertib phosphate (Synonyms: INCB053914 phosphate)

Customer Review

Other Forms of Uzansertib phosphate:

Uzansertib phosphate Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Pim Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Uzansertib phosphate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Uzansertib phosphate Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report