XL019

Name: XL019
Brand: MedChemExpress
SKU: HY-13775
Rating: 5.0 (5 reviews)

Cat. No.: HY-13775 Purity: 99.65%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC₅₀s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.

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

XL019 Chemical Structure

CAS No. : 945755-56-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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

Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE XL019

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View All Isoforms

JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

JAK2

2.2 nM (IC₅₀)

JAK3

214.2 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	7.34 μM Compound: XL019; 3	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 30243158]
MCF7	IC₅₀	27.2 μM Compound: XL019; 3	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30243158]
MDA-MB-231	IC₅₀	9.67 μM Compound: XL019; 3	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 30243158]
PC-3	IC₅₀	14.9 μM Compound: XL019; 3	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 30243158]

In Vivo

XL019 (100-300 mg/kg; p.o.; twice daily for 14 days) inhibits HEL.92.1.7 xenograft tumor growth^[1].
XL019 (10 mg/kg) treatment shows that the?C_max, t_1/2?and V_d were?5.24 μM,?1.94 hours,?5.319 L/kg,?respectively^[1].

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

Animal Model:	Female nude mice (HEL.92.1.7 xenograft tumors)^[1]
Dosage:	100, 200, 300 mg/kg
Administration:	p.o.; twice daily for 14 days
Result:	Inhibition of HEL.92.1.7 xenograft tumor growth.

Animal Model:	Mouse^[1]
Dosage:	10 mg/kg
Administration:	p.o.(Pharmacokinetic Analysis)
Result:	The C_max, t_1/2 and V_d were 5.24 μM, 1.94 hours, and 5.319 L/kg, respectively.

Clinical Trial

Molecular Weight

444.53

Formula

C₂₅H₂₈N₆O₂

CAS No.

945755-56-6

Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C([C@H]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2

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 : 25 mg/mL (56.24 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	2.2496 mL	11.2478 mL	22.4957 mL
5 mM	0.4499 mL	2.2496 mL	4.4991 mL
10 mM	0.2250 mL	1.1248 mL	2.2496 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 (5.62 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.

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: 99.65%

Select Batch:

Data Sheet (273 KB) SDS (418 KB)

COA (244 KB) HNMR (412 KB) RP-HPLC (259 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Forsyth T, et al. SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2496 mL	11.2478 mL	22.4957 mL	56.2392 mL
	5 mM	0.4499 mL	2.2496 mL	4.4991 mL	11.2478 mL
	10 mM	0.2250 mL	1.1248 mL	2.2496 mL	5.6239 mL
	15 mM	0.1500 mL	0.7499 mL	1.4997 mL	3.7493 mL
	20 mM	0.1125 mL	0.5624 mL	1.1248 mL	2.8120 mL
	25 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2496 mL
	30 mM	0.0750 mL	0.3749 mL	0.7499 mL	1.8746 mL
	40 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4060 mL
	50 mM	0.0450 mL	0.2250 mL	0.4499 mL	1.1248 mL

XL019 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:

XL019945755-56-6XL 019XL-019JAKApoptosisJanus kinaseselectiveoraltumorphosphorylationantitumor,HEL.92.1.7cellsInhibitorinhibitorinhibit

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XL019

Customer Review

XL019 Related Antibodies

5 Publications Citing Use of MCE XL019

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

XL019 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report