TC-A 2317 hydrochloride

Name: TC-A 2317 hydrochloride
Brand: MedChemExpress
SKU: HY-103266
Rating: 4.5 (1 reviews)

Cat. No.: HY-103266 Purity: 99.57%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (K_i=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (K_i=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity.

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

TC-A 2317 hydrochloride Chemical Structure

CAS No. : 1245907-03-2

Size	Price	Stock	Quantity
5 mg	USD 236	In-stock	Estimated Time of Arrival: December 31
10 mg		Get quote
50 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

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View All Aurora Kinase Isoform Specific Products:

View All Isoforms

Aurora Kinase Aurora A Aurora B Aurora C

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Aurora A

1.2 nM (Ki)

Aurora B

101 nM (Ki)

In Vitro

TC-A 2317 hydrochloride (Compound 6) inhibits proliferation of HCT116 cells with an IC₅₀ of 115 nM^[1].

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

In Vivo

TC-A 2317 hydrochloride is effective in antitumor mice model without decrease of body weight^[1].
TC-A 2317 hydrochloride shows good PK profile; C_max value is 4930 nM (T_max=1.2 h) and serum concentration after 24 h is 52 nM (T_1/2=3.3 h) at 30 mg/kg po in rats^[1].

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

Animal Model:	HCT-116 Xenograft mice mode^[1]
Dosage:	P.o.; daily for 14 days
Administration:	30 mg/kg
Result:	Growth of tumor was inhibited by 59% after 14 days.

Molecular Weight

392.93

Formula

C₁₉H₂₉ClN₆O

CAS No.

1245907-03-2

Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(C)C=C(NC2=NNC(C)=C2)N=C1NC(C)CCCC(C)(O)C.[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 : 100 mg/mL (254.50 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	2.5450 mL	12.7249 mL	25.4498 mL
5 mM	0.5090 mL	2.5450 mL	5.0900 mL
10 mM	0.2545 mL	1.2725 mL	2.5450 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.

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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 (6.36 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 (6.36 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 (6.36 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).

*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: 99.57%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

COA (246 KB) HNMR (143 KB) RP-HPLC (164 KB) LCMS (294 KB)

Handling Instructions (2659 KB)

References

[1]. Ando R, et al. 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. Bioorg Med Chem Lett. 2010;20(15):4709-4711. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5450 mL	12.7249 mL	25.4498 mL	63.6246 mL
	5 mM	0.5090 mL	2.5450 mL	5.0900 mL	12.7249 mL
	10 mM	0.2545 mL	1.2725 mL	2.5450 mL	6.3625 mL
	15 mM	0.1697 mL	0.8483 mL	1.6967 mL	4.2416 mL
	20 mM	0.1272 mL	0.6362 mL	1.2725 mL	3.1812 mL
	25 mM	0.1018 mL	0.5090 mL	1.0180 mL	2.5450 mL
	30 mM	0.0848 mL	0.4242 mL	0.8483 mL	2.1208 mL
	40 mM	0.0636 mL	0.3181 mL	0.6362 mL	1.5906 mL
	50 mM	0.0509 mL	0.2545 mL	0.5090 mL	1.2725 mL
	60 mM	0.0424 mL	0.2121 mL	0.4242 mL	1.0604 mL
	80 mM	0.0318 mL	0.1591 mL	0.3181 mL	0.7953 mL
	100 mM	0.0254 mL	0.1272 mL	0.2545 mL	0.6362 mL