AT9283

Name: AT9283
Brand: MedChemExpress
SKU: HY-50514
Rating: 5.0 (5 reviews)

Cat. No.: HY-50514 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC₅₀s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.

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

AT9283 Chemical Structure

CAS No. : 896466-04-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 131	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 131	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 211	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 551	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 800	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 5 publication(s) in Google Scholar

Other Forms of AT9283:

AT9283 hydrochloride Get quote
AT9283 lactic acid Get quote

5 Publications Citing Use of MCE AT9283

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

View All Isoforms

JAK1 JAK2 JAK3 Tyk2 JAK

View All Aurora Kinase Isoform Specific Products:

View All Isoforms

Aurora Kinase Aurora A Aurora B Aurora C

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Aurora A

3 nM (IC₅₀)

Aurora B

3 nM (IC₅₀)

JAK3

1.1 nM (IC₅₀)

JAK2

1.2 nM (IC₅₀)

ABL(T315I)

4 nM (IC₅₀)

Flt-3

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.512 μM Compound: AT-9283	Antitumor activity against human A549 cells after 72 hrs by MTT assay Antitumor activity against human A549 cells after 72 hrs by MTT assay	[PMID: 23664099]
BaF3	IC₅₀	11 nM Compound: AT9283	Antiproliferative activity against mouse BaF3 cells harbouring ABL-T315I mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring ABL-T315I mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35551036]
BaF3	IC₅₀	13 nM Compound: AT9283	Antiproliferative activity against mouse BaF3 cells harbouring wild type ABL assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring wild type ABL assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35551036]
HCT-116	IC₅₀	0.09 μM Compound: AT9283	Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by CCK8 assay	[PMID: 33109396]
HCT-116	IC₅₀	12 nM Compound: 16, AT9283	Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay	[PMID: 19143567]
HT-29	IC₅₀	0.383 μM Compound: AT-9283	Antitumor activity against human HT-29 cells after 72 hrs by MTT assay Antitumor activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23664099]
HUVEC	IC₅₀	1.793 μM Compound: AT9283	Cytotoxicity against HUVEC assessed as reduction in cell growth measured after 72 hrs by CCK8 assay Cytotoxicity against HUVEC assessed as reduction in cell growth measured after 72 hrs by CCK8 assay	[PMID: 33109396]
K562	IC₅₀	0.748 μM Compound: AT9283	Antiproliferative activity against human K562 cells assessed as reduction in cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as reduction in cell growth measured after 72 hrs by CCK8 assay	[PMID: 33109396]
K562	IC₅₀	1.6 μM Compound: AT-9283	Antitumor activity against human K562 cells after 72 hrs by MTT assay Antitumor activity against human K562 cells after 72 hrs by MTT assay	[PMID: 23664099]
LoVo	IC₅₀	0.553 μM Compound: AT-9283	Antitumor activity against human LoVo cells after 72 hrs by MTT assay Antitumor activity against human LoVo cells after 72 hrs by MTT assay	[PMID: 23664099]
U-937	IC₅₀	6.7 μM Compound: AT-9283	Antitumor activity against human U937 cells after 72 hrs by MTT assay Antitumor activity against human U937 cells after 72 hrs by MTT assay	[PMID: 23664099]

In Vitro

AT9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC₅₀ of 30 nM. Furthermore, AT9283 also produces the potent inhibition on HCT116 colony formation^[1].
AT9283 induces apoptosis in a dose and time dependent manner and inhibits cell proliferation with an IC₅₀ < 1 μM in B-NHL cell lines^[2].
AT9283 inhibits growth, induces dose dependent cytotoxicity, and inhibits STAT3 signaling pathway in MM cell lines. T9283 inhibits phospho Histone H3 and phospho Aurora A at Thr 288. AT9283 increases G2/M phase and induces apoptosis of MM cells in a time-dependent manner^[3].

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

In Vivo

In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, AT9283 also exhibits a significantly longer half-life in tumors (2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice^[1].
AT9283 (15 mg/kg) and docetaxel (10 mg/kg) alone has modest anti-tumor activity. T9283 at 20 mg/kg and AT9283 (15 or 20 mg/kg) plus docetaxel (10 mg/kg) demonstrate a statistically significant tumor growth inhibition and enhance survival inmouse xenograft model of mantle cell lymphoma^[2].
AT9283 (45 mg/kg, i.p.) inhibits tumor growth in mice. Two cycles of AT9283 45 mg/kg 14 hours after drug administration confirm decreased expression of phospho-Histone H3 and Aurora B in treated animals^[3].

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

Clinical Trial

Molecular Weight

381.43

Formula

C₁₉H₂₃N₇O₂

CAS No.

896466-04-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1CC1)NC2=CNN=C2C3=NC4=CC=C(C=C4N3)CN5CCOCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (262.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6217 mL	13.1086 mL	26.2171 mL
5 mM	0.5243 mL	2.6217 mL	5.2434 mL
10 mM	0.2622 mL	1.3109 mL	2.6217 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.5 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).

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: 99.67%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (248 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Howard S, et al. Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity. Journal of Medicinal Chemistry (2009), 52(2), 379-388. [Content Brief]

[2]. Qi W, et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int J Cancer. 2012 Jun 15;130(12):2997-3005. [Content Brief]

[3]. Santo L, et al. Antimyeloma activity of a multitargeted kinase inhibitor, AT9283, via potent Aurora kinase and STAT3 inhibition either alone or in combination with lenalidomide. Clin Cancer Res. 2011 May 15;17(10):3259-71 [Content Brief]

Cell Assay ^[2]	Lymphoma cells are seeded at 8,000 per well in 96-well culture plates and allowed to grow for 24 hr followed by the desired treatment with increasing concentrations of the indicated agents for 4 days. Viable cell densities are determined using a CellTiter 96 Cell Proliferation Assay. The IC₅₀ values are estimated by Calcusyn software. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	SCID mice are injected with 1×10⁷ Granta-519 MCL cells subcutaneously into the right hind flank. When tumors reached a volume of appr 60-100 mm³, mice are divided randomly (pair-matched) into six test groups with 12 mice per cohort: control group (saline), AT9283 (15 mg/kg IP Q1D, 5 days a week × 3 weeks) group, AT9283 (20 mg/kg IP Q1D, 5 days a week × 3 weeks) group, docetaxel (10 mg/kg IV Q1W × 3 weeks) group, AT9283 (15 mg/kg IP Q1D, 5 days a week × 3 weeks) + docetaxel (10 mg/kg IV Q1W × 3 weeks) group and AT9283 (20 mg/kg IP Q1D, 5 days a week × 3 weeks) + docetaxel (10 mg/kg IV Q1W × 3 weeks) group. The length (L) and width (W) of the subcutaneous tumors are measured by calipers and the tumor volume (TV) is calculated as: TV=(L × W²)/2. Mice are sacrificed at the end of study and overall survival for each cohort is analyzed by Kaplan–Meier method. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Howard S, et al. Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity. Journal of Medicinal Chemistry (2009), 52(2), 379-388. [Content Brief] [2]. Qi W, et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int J Cancer. 2012 Jun 15;130(12):2997-3005. [Content Brief] [3]. Santo L, et al. Antimyeloma activity of a multitargeted kinase inhibitor, AT9283, via potent Aurora kinase and STAT3 inhibition either alone or in combination with lenalidomide. Clin Cancer Res. 2011 May 15;17(10):3259-71 [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.6217 mL	13.1086 mL	26.2171 mL	65.5428 mL
	5 mM	0.5243 mL	2.6217 mL	5.2434 mL	13.1086 mL
	10 mM	0.2622 mL	1.3109 mL	2.6217 mL	6.5543 mL
	15 mM	0.1748 mL	0.8739 mL	1.7478 mL	4.3695 mL
	20 mM	0.1311 mL	0.6554 mL	1.3109 mL	3.2771 mL
	25 mM	0.1049 mL	0.5243 mL	1.0487 mL	2.6217 mL
	30 mM	0.0874 mL	0.4370 mL	0.8739 mL	2.1848 mL
	40 mM	0.0655 mL	0.3277 mL	0.6554 mL	1.6386 mL
	50 mM	0.0524 mL	0.2622 mL	0.5243 mL	1.3109 mL
	60 mM	0.0437 mL	0.2185 mL	0.4370 mL	1.0924 mL
	80 mM	0.0328 mL	0.1639 mL	0.3277 mL	0.8193 mL
	100 mM	0.0262 mL	0.1311 mL	0.2622 mL	0.6554 mL

AT9283 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.

Keywords:

AT9283896466-04-9AT 9283AT-9283JAKAurora KinaseBcr-AblFLT3ApoptosisAutophagyJanus kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
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.

AT9283

Customer Review

Other Forms of AT9283:

AT9283 Related Antibodies

5 Publications Citing Use of MCE AT9283

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

View All Aurora Kinase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

AT9283 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AT9283 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report