2. Protein Tyrosine Kinase/RTK
    Apoptosis
  3. Bcr-Abl
    Apoptosis
  4. Adaphostin

Adaphostin  (Synonyms: NSC 680410)

Cat. No.: HY-103275 Purity: 99.02%
COA Handling Instructions

Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells.

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

Adaphostin Chemical Structure

Adaphostin Chemical Structure

CAS No. : 241127-58-2

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Based on 1 publication(s) in Google Scholar

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Description

Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells[1][2][3].

In Vitro

Adaphostin down-regulates p210bcr/abl in K562 cells and inhibits granulocyte colony formation in chronic myelogenous leukemia (CML) specimens at lower concentrations without enhanced toxicity in normal progenitors[1].
Adaphostin-induced p53 up-regulation, DNA strand breaks, and ROS production in ML-1 cells is inhibited by N-acetylcysteine (NAC)[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

393.48

Appearance

Solid

Formula

C24H27NO4
CAS No.
SMILES

O=C(C(C=C1)=CC=C1NCC(C=C2O)=C(C=C2)O)OC3(C[[email protected]](C4)C5)C[[email protected]]5C[[email protected]]4C3
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 (127.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.02%

COA (247 KB) HNMR (252 KB) LCMS (259 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Adaphostin241127-58-2NSC 680410NSC680410NSC-680410Bcr-AblApoptosischronic myelogenous leukemiaCMLp210Bcr/ablROSmyeloidtyrosine kinaseInhibitorinhibitorinhibit

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