Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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Adaphostin (NSC-680410) is the adamantyl ester of AG957, acting as a novel and potent activator of Fas-mediated death pathway in Bcr/Abl-positive leukaemia. It also causes apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM) as a p210bcr/abl inhibitor (IC50=14 μM).
ln Vitro |
Adaphostin inhibits granulocyte colony formation in specimens of chronic myelogenous leukemia (CML) at lower concentrations without increasing toxicity in normal progenitors and down-regulates p210bcr/abl in K562 cells[1].
N-acetylcysteine (NAC) inhibits adipostin-induced p53 up-regulation, DNA strand breaks, and ROS production in ML-1 cells[4]. |
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References |
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Molecular Formula |
C24H27NO4
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Molecular Weight |
393.47500
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Exact Mass |
393.194
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Elemental Analysis |
C, 73.26; H, 6.92; N, 3.56; O, 16.26
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CAS # |
241127-58-2
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Related CAS # |
241127-58-2
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PubChem CID |
387042
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Appearance |
Off-white to light brown solid powder
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Density |
1.33g/cm3
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Boiling Point |
606.2ºC at 760mmHg
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Flash Point |
320.4ºC
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Vapour Pressure |
2.73E-15mmHg at 25°C
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Index of Refraction |
1.661
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LogP |
4.991
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Hydrogen Bond Donor Count |
3
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
6
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Heavy Atom Count |
29
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Complexity |
558
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Defined Atom Stereocenter Count |
0
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SMILES |
OC1=CC=C(O)C(CNC2=CC=C(C(OC34CC5CC(C3)CC(C5)C4)=O)C=C2)=C1
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InChi Key |
YJZSUCFGHXQWDM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H27NO4/c26-21-5-6-22(27)19(10-21)14-25-20-3-1-18(2-4-20)23(28)29-24-11-15-7-16(12-24)9-17(8-15)13-24/h1-6,10,15-17,25-27H,7-9,11-14H2
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Chemical Name |
1-adamantyl 4-[(2,5-dihydroxyphenyl)methylamino]benzoate
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Synonyms |
Adaphostin
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~50 mg/mL (~127.1 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5414 mL | 12.7071 mL | 25.4143 mL | |
5 mM | 0.5083 mL | 2.5414 mL | 5.0829 mL | |
10 mM | 0.2541 mL | 1.2707 mL | 2.5414 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Cells lacking Bcr/abl are susceptible to adaphostin-induced apoptosis. Blood . 2003 Dec 15;102(13):4512-9. td> |
Adaphostin-induced p53 up-regulation, DNA strand breaks, and ROS production in ML-1 cells is inhibited by NAC. Blood . 2003 Dec 15;102(13):4512-9. td> |
NAC inhibits adaphostin-induced ROS production and cytotoxicity in K562 cells. Blood . 2003 Dec 15;102(13):4512-9. td> |
Antiproliferative/cytotoxic activity of adaphostin against chronic myeloid leukemia (CML) and acute myeloid leukemia (AML) cell lines. Cancer Sci . 2006 Sep;97(9):952-60. td> |
(A) Induction of apoptosis in AML2 and KBM7 cells by adaphostin. Cancer Sci . 2006 Sep;97(9):952-60. td> |
Induction of apoptosis after imatinib or adaphostin exposure in Ph-positive cell lines. Cancer Sci . 2006 Sep;97(9):952-60. td> |