Art. -Nr.: HY-126686

Mal-Phe-C4-VC-PAB-MMAE

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Mal-Phe-C4-VC-PAB-MMAE is a drug-linker conjugate for ADC composed of MMAE conjugated to the Mal-Phe-C4-VC-PAB linker. Mal-Phe-C4-VC-PAB-MMAE can be used to synthesize antibody-drug conjugates targeting ROR1, and the resulting ADC exhibits in vitro tumor cell proliferation inhibitory activity. Mal-Phe-C4-VC-PAB-MMAE is applicable to research on cancers expressing ROR1.

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Reinheit: 99.54%
CAS. Nr.: 2259318-51-7
Formel: C₇₂H₁₀₅N₁₁O₁₅
Molecular Weight:1364.67

Speicherung:

-20°C, sealed storage, away from moisture and light

* The compound is unstable in solutions, freshly prepared is recommended.

Mal-Phe-C4-VC-PAB-MMAE Chemical Structure

CAS. Nr.: 2259318-51-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Auristatin

Alle Drug-Linker Conjugates for ADC Isoform-spezifische Produkte anzeigen :

In Vitro

Mal-Phe-C4-VC-PAB-MMAE conjugated ADC-M (0.0045-10 μM; 72 h) exhibits potent antiproliferative activity against ROR1-positive Mino mantle cell lymphoma cells (EC₅₀ = 15.8 nM), MDA-MB-468 triple-negative breast cancer cells (EC₅₀ = 53.1 nM), and MCF-7 estrogen-positive breast cancer cells (EC₅₀ = 164.1 nM)^[1].
Mal-Phe-C4-VC-PAB-MMAE conjugated ADC-M undergoes rapid internalization into ROR1-positive Jeko-1 mantle cell lymphoma cells and MDA-MB-231 triple-negative breast cancer cells after binding to the cell surface ROR1 antigen^[1].

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

In Vivo

Mal-Phe-C4-VC-PAB-MMAE conjugated ADC-M (1-5 mg；every 4 days, intravenous administration) achieves partial tumor growth inhibition and significant tumor regression at two distinct dosages in Jeko-1 human mantle cell xenograft animal models^[1].

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

Chemical Information

CAS. Nr. 2259318-51-7
Appearance Solid
Molecular Weight 1364.67
Formel C₇₂H₁₀₅N₁₁O₁₅
Color White to light yellow
SMILES

O[C@@H](C1=CC=CC=C1)[C@@H](C)NC([C@H](C)[C@H]([C@@]2([H])N(CCC2)C(C[C@@H](OC)[C@@]([C@@H](C)CC)([H])N(C)C([C@H](C(C)C)NC([C@H](C(C)C)N(C)C(OCC3=CC=C(NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC(CCCC4=CC=C(N5C(C=CC5=O)=O)C=C4)=O)=O)=O)C=C3)=O)=O)=O)=O)OC)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture and light

* The compound is unstable in solutions, freshly prepared is recommended.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 200 mg/mL (146.56 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.7328 mL

3.6639 mL

7.3278 mL

5 mM

0.1466 mL

0.7328 mL

1.4656 mL

10 mM

0.0733 mL

0.3664 mL

0.7328 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 5 mg/mL (3.66 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (3.66 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lannutti B, et al. Ror1 antibody immunoconjugates. WO2018237335A1, World Intellectual Property Organization, 2018.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.7328 mL	3.6639 mL	7.3278 mL	18.3194 mL
	5 mM	0.1466 mL	0.7328 mL	1.4656 mL	3.6639 mL
	10 mM	0.0733 mL	0.3664 mL	0.7328 mL	1.8319 mL
	15 mM	0.0489 mL	0.2443 mL	0.4885 mL	1.2213 mL
	20 mM	0.0366 mL	0.1832 mL	0.3664 mL	0.9160 mL
	25 mM	0.0293 mL	0.1466 mL	0.2931 mL	0.7328 mL
	30 mM	0.0244 mL	0.1221 mL	0.2443 mL	0.6106 mL
	40 mM	0.0183 mL	0.0916 mL	0.1832 mL	0.4580 mL
	50 mM	0.0147 mL	0.0733 mL	0.1466 mL	0.3664 mL
	60 mM	0.0122 mL	0.0611 mL	0.1221 mL	0.3053 mL
	80 mM	0.0092 mL	0.0458 mL	0.0916 mL	0.2290 mL
	100 mM	0.0073 mL	0.0366 mL	0.0733 mL	0.1832 mL

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Mal-Phe-C4-VC-PAB-MMAE

Alle Drug-Linker Conjugates for ADC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mal-Phe-C4-VC-PAB-MMAE Related Classifications

HY-126686 Related Classifications