AT7519 Hydrochloride

Name: AT7519 Hydrochloride
Brand: MedChemExpress
SKU: HY-50943
Rating: 5.0 (12 reviews)

Cat. No.: HY-50943 Purity: 99.42%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC₅₀s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

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

AT7519 Hydrochloride Chemical Structure

CAS No. : 902135-91-5

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 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 209	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 275	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 12 publication(s) in Google Scholar

Other Forms of AT7519 Hydrochloride:

AT7519 In-stock
AT7519 TFA In-stock

12 Publications Citing Use of MCE AT7519 Hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC₅₀s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

IC₅₀ & Target^[2]

CDK9/Cyclin T

10 nM (IC₅₀)

CDK5/p35

13 nM (IC₅₀)

cdk2/cyclin A

47 nM (IC₅₀)

Cdk4/cyclin D1

100 nM (IC₅₀)

cdk6/cyclin D3

170 nM (IC₅₀)

Cdk1/cyclin B

210 nM (IC₅₀)

CDK7/Cyclin H/MAT1

2400 nM (IC₅₀)

GSK3β

89 nM (IC₅₀)

In Vitro

AT7519 (0-4 μM) results in dose-dependent cytotoxicity with IC₅₀s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells^[1]. AT7519 (250 nM) inhibits cell cycle progression in human tumor cell lines. AT7519 also induces apoptosis of human tumor cell lines^[2]. AT7519 (100-700 nM) induces apoptosis in leukemia cell lines. AT7519 also inhibits transcription in human tumor cell lines. Furthermore, AT7519 inhibits RNA polymerase II and reduces antiapoptotic protein levels^[3].

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

In Vivo

AT7519 inhibits tumor growth in a human MM xenograft mouse model^[1]. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice^[2].

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

Clinical Trial

Molecular Weight

418.71

Formula

C₁₆H₁₈Cl₃N₅O₂

CAS No.

902135-91-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C(Cl)=CC=C1)=C1Cl)NC2=CNN=C2C(NC3CCNCC3)=O.[H]Cl

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 : ≥ 300 mg/mL (716.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 8.33 mg/mL (19.89 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3883 mL	11.9414 mL	23.8829 mL
5 mM	0.4777 mL	2.3883 mL	4.7766 mL
10 mM	0.2388 mL	1.1941 mL	2.3883 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.42%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (258 KB) LCMS (276 KB)

Handling Instructions (2659 KB)

References

[1]. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36. [Content Brief]

[2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. [Content Brief]

[3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8. [Content Brief]

Cell Assay ^[1]	AT7519's effects on viability of MM cell lines, primary MM cells, and PBMNCs is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT) dye absorbance. DNA synthesis is measured by tritiated thymidine uptake (3H-TdR). MM cells (2-3 × 10⁴ cells/well) are incubated in 96-well culture plates with media and different concentrations of AT7519 and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 or 48 h at 37°C and 3H-TdR incorporation is measured. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	To evaluate the in vivo anti-MM activity of AT7519, male SCID mice are inoculated subcutaneously with 5×10⁶ MM.1S cells in 100 μL serum-free RPMI 1640 medium. When tumors are measurable, mice are treated intraperitoneally (IP) with vehicle or AT7519 dissolved in saline 0.9%. The first group of 10 mice is treated with 15 mg/kg once a day for five days for 2 weeks, and the second group is treated with 15 mg/kg once a day three times a week for four consecutive weeks. The control group receives the carrier alone at the same schedule. Tumor size is measured every alternate day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V= 0.5 a × b² (a= long diameter of the tumor, b= short diameter of the tumor). Animals are sacrificed when the tumor reaches 2 cm³ or when the tumor is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36. [Content Brief] [2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. [Content Brief] [3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.3883 mL	11.9414 mL	23.8829 mL	59.7072 mL
	5 mM	0.4777 mL	2.3883 mL	4.7766 mL	11.9414 mL
	10 mM	0.2388 mL	1.1941 mL	2.3883 mL	5.9707 mL
	15 mM	0.1592 mL	0.7961 mL	1.5922 mL	3.9805 mL
DMSO	20 mM	0.1194 mL	0.5971 mL	1.1941 mL	2.9854 mL
	25 mM	0.0955 mL	0.4777 mL	0.9553 mL	2.3883 mL
	30 mM	0.0796 mL	0.3980 mL	0.7961 mL	1.9902 mL
	40 mM	0.0597 mL	0.2985 mL	0.5971 mL	1.4927 mL
	50 mM	0.0478 mL	0.2388 mL	0.4777 mL	1.1941 mL
	60 mM	0.0398 mL	0.1990 mL	0.3980 mL	0.9951 mL
	80 mM	0.0299 mL	0.1493 mL	0.2985 mL	0.7463 mL
	100 mM	0.0239 mL	0.1194 mL	0.2388 mL	0.5971 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.