NAMPT inhibitor-linker 2

Name: NAMPT inhibitor-linker 2
Brand: MedChemExpress
SKU: HY-112616
Rating: 4.5 (1 reviews)

Cat. No.: HY-112616 Purity: 98.11%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC₅₀s of <7 pM and 40 pM, respectively.

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

NAMPT inhibitor-linker 2 Chemical Structure

CAS No. : 2241014-82-2

Size	Price	Stock	Quantity
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 960	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1540	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2460	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Traditional Cytotoxic Agents

In Vitro

ADC-4 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC₅₀s of <7 pM and 40 pM, respectively^[1].
ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	GIST-T1 cells
Concentration:	0.1 pM-10 nM
Incubation Time:	144 hours
Result:	Inhibited the cell proliferation of GIST-T1 cells at 0.01-10 nM, and the inhibition remained unchanged after 1 nM.

In Vivo

ADC-4 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells^[1].

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

Animal Model:	Female scid-beige (SCID bg) mice^[1]
Dosage:	20 mg/kg
Administration:	A single intravenous injection (i.v.) for 28 days
Result:	Significantly inhibited the growth of tumor in mice.

Molecular Weight

624.66

Formula

C₃₄H₃₃FN₆O₅

CAS No.

2241014-82-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=CC(NC([C@@H]2[C@H](C2)C3=CN=CC=C3)=O)=CC=C1CNC(C4=CC=C(N5CCN(C(CCN6C(C=CC6=O)=O)=O)CC5)C=C4)=O

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 : 50 mg/mL (80.04 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	1.6009 mL	8.0044 mL	16.0087 mL
5 mM	0.3202 mL	1.6009 mL	3.2017 mL
10 mM	0.1601 mL	0.8004 mL	1.6009 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 (4.00 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 (4.00 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 (4.00 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: 98.11%

Select Batch:

Data Sheet (271 KB) SDS (251 KB)

COA (244 KB) HNMR (286 KB) RP-HPLC (164 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Karpov AS, et al. Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates. ACS Med Chem Lett. 2018 Jun 28;9(8):838-842. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.6009 mL	8.0044 mL	16.0087 mL	40.0218 mL
	5 mM	0.3202 mL	1.6009 mL	3.2017 mL	8.0044 mL
	10 mM	0.1601 mL	0.8004 mL	1.6009 mL	4.0022 mL
	15 mM	0.1067 mL	0.5336 mL	1.0672 mL	2.6681 mL
	20 mM	0.0800 mL	0.4002 mL	0.8004 mL	2.0011 mL
	25 mM	0.0640 mL	0.3202 mL	0.6403 mL	1.6009 mL
	30 mM	0.0534 mL	0.2668 mL	0.5336 mL	1.3341 mL
	40 mM	0.0400 mL	0.2001 mL	0.4002 mL	1.0005 mL
	50 mM	0.0320 mL	0.1601 mL	0.3202 mL	0.8004 mL
	60 mM	0.0267 mL	0.1334 mL	0.2668 mL	0.6670 mL
	80 mM	0.0200 mL	0.1001 mL	0.2001 mL	0.5003 mL