Apatinib-d₈ hydrochloride

Name: Apatinib-d 8 hydrochloride
Brand: MedChemExpress
SKU: HY-13342S
Rating: 5.0 (1 reviews)

Cat. No.: HY-13342S Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Apatinib-d₈ (hydrochloride) is the deuterium labeled Apatinib hydrochloride[1].

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

Apatinib-d<sub>8</sub> hydrochloride Chemical Structure

Apatinib-d₈ hydrochloride Chemical Structure

CAS No. : 2468771-44-8

Size	Price	Stock	Quantity
1 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 710	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1150	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 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 Apatinib-d₈ hydrochloride:

Apatinib In-stock

1 Publications Citing Use of MCE Apatinib-d₈ hydrochloride

•bioRxiv. 2024 September 01.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

Apatinib-d₈ (hydrochloride) is the deuterium labeled Apatinib hydrochloride[1].

In Vitro

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

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

Molecular Weight

441.98

Formula

C₂₄H₁₆D₈ClN₅O

CAS No.

2468771-44-8

Unlabeled CAS

1218779-75-9

Appearance

Solid

Color

White to off-white

SMILES

C(#N)C1(C(C(C(C1([2H])[2H])([2H])[2H])([2H])[2H])([2H])[2H])C2=CC=C(NC(=O)C3=C(NCC=4C=CN=CC4)N=CC=C3)C=C2.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (226.25 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	2.2625 mL	11.3127 mL	22.6255 mL
5 mM	0.4525 mL	2.2625 mL	4.5251 mL
10 mM	0.2263 mL	1.1313 mL	2.2625 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. 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: ≥ 2.5 mg/mL (5.66 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 (5.66 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 (5.66 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: 98.00%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (255 KB) HNMR (234 KB) RP-HPLC (287 KB) Elemental Analysis Report (114 KB)

Handling Instructions (2659 KB)

References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / DMSO	1 mM	2.2625 mL	11.3127 mL	22.6255 mL	56.5636 mL
	5 mM	0.4525 mL	2.2625 mL	4.5251 mL	11.3127 mL
	10 mM	0.2263 mL	1.1313 mL	2.2625 mL	5.6564 mL
	15 mM	0.1508 mL	0.7542 mL	1.5084 mL	3.7709 mL
	20 mM	0.1131 mL	0.5656 mL	1.1313 mL	2.8282 mL
	25 mM	0.0905 mL	0.4525 mL	0.9050 mL	2.2625 mL
	30 mM	0.0754 mL	0.3771 mL	0.7542 mL	1.8855 mL
	40 mM	0.0566 mL	0.2828 mL	0.5656 mL	1.4141 mL
	50 mM	0.0453 mL	0.2263 mL	0.4525 mL	1.1313 mL
	60 mM	0.0377 mL	0.1885 mL	0.3771 mL	0.9427 mL
	80 mM	0.0283 mL	0.1414 mL	0.2828 mL	0.7070 mL
	100 mM	0.0226 mL	0.1131 mL	0.2263 mL	0.5656 mL