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Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222) ADC Cytotoxin inhibitor

Name: Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222)
Brand: Selleck Chemicals
SKU: S2447
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S2447

Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222, Antibiotic C 15003P3) is a potent inhibitor of tubulin polymerization with IC50 of 3.4 μM.

Chemical Structure

Molecular Weight: 635.14

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.28%

99.28

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Chemical Information, Storage & Stability

Molecular Weight	635.14	Formula	C₃₂H₄₃ClN₂O₉	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	66584-72-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Antibiotic C 15003P3			Smiles	CC1C2CC(C(C=CC=C(CC3=CC(=C(C(=C3)OC)Cl)N(C(=O)CC(C4(C1O4)C)OC(=O)C(C)C)C)C)OC)(NC(=O)O2)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (157.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 55 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (7.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (7.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (1.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Ansamitocin p-3 does not inhibit the growth of bacteria, but very markedly inhibits the growth of eukaryotic organisms.
In vitro	Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222) at 5 μM completely inhibits the polymerization of tubulin isolated from bovine brains, but in contrast to VCR, this compound at a high concentration of 80 μM does not leads to the aggregation of tubulin. It at 16 μM also potently depolymerizes the polymerized tubulin (IC50 = 3.8 μM). The addition of Ansamitocin p-3 to culture cells blocks the morphological alteration of AC cells from fibroepithelioid to a glial cell type caused by the exposure to a certain concentration of dibutyryl cyclic adenosine 3':5'-monophosphate. In addition, it at 16 nM causes the well-defined network of cytoplasmic microtubules of A31 cells rapidly dispersed. Short-term treatment with this compound also inhibits the synthesis of DNA in A31 cells or KB cells. These results confirm that it acts by interfering with the microtubule assembly system, thus resulting in an inhibition of mitotic spindle fiber formation and, ultimately, cytokilling. ^[1] This compound displays potent cytotoxicity against A-549, HT-29, and MCF-7 cells in a dose-dependent manner with ED50 of 4 ×10^-7, 4 × 10^-7, and 2 × 10^-6 μg/mL, respectively. ^[2] It also exhibits cytotoxicity against HCT-116 cells with a much low EC50 of 0.081 nM. ^[3] Ansamitocin p-3 enhances the effect of radiation both in Drosophila cells and human cancer cells in a p53 dependent manner. ^[4]
Kinase Assay	Polymerization inhibition assay
Kinase Assay	After the addition of 100 μL of various concentrations of Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222) solution (GTP minus MES buffer) or 1 M Tris buffer, pH 8.4 (for blank), to 400 μL of bovine tubulin solution (1 mg/mL in cold MES buffer), maintained at 0 °C for 10 to 15 minutes, the mixture is warmed in a water bath at 37 °C for 30 to 60 minutes. The polymerization of tubulin is followed by an increase in turbidity of the mixture during warming. The turbidity measurement is performed at 460 nm with a Hitachi type 101 spectrophotometer.
In vivo	Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222) treatment (>1 μg) significantly suppresses the growth of leukemia SN36, and induces an increased arrest in metaphase of P388 leukemia cells. At 25 μg/kg/day, it significantly prolongs the survival time of mice bearing i.p. B16 melanoma by 130%. This compound also significantly prolongs the survival time of mice bearing Ehrlich ascites carcinoma, Sarcoma 180, and P815 mastocytoma, while slightly prolonging the survival time of mice bearing ascites MOPC-104E myeloma, leukemia L1210, and leukemia C1498. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/6245801/ [2] https://pubmed.ncbi.nlm.nih.gov/2298279/ [3] https://pubmed.ncbi.nlm.nih.gov/16314405/ [4] https://pubmed.ncbi.nlm.nih.gov/21504911/ [5] https://pubmed.ncbi.nlm.nih.gov/24124473/

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