2. Apoptosis
  3. MDM-2/p53
  4. ASTX295

ASTX295 is a selective mouse double minute 2 (MDM2) antagonist with an IC50 value of <1 nM. ASTX295 specifically blocks the interaction between MDM2 and p53, reactivating wild-type (WT) TP53, and then inducing the expression of related transcriptional targets, leading to cell death and cell cycle arrest. ASTX295 is promising for research of lymphoid malignancies, such as diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), and T-cell lymphoma.

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ASTX295

ASTX295 Chemical Structure

CAS No. : 2093449-12-6

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Description

ASTX295 is a selective mouse double minute 2 (MDM2) antagonist with an IC50 value of <1 nM. ASTX295 specifically blocks the interaction between MDM2 and p53, reactivating wild-type (WT) TP53, and then inducing the expression of related transcriptional targets, leading to cell death and cell cycle arrest. ASTX295 is promising for research of lymphoid malignancies, such as diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), and T-cell lymphoma[1].

Clinical Trial
Molecular Weight

630.53

Formula

C33H34Cl2FNO6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CO[C@](C(C(C1=O)=C2)=C(F)C=C2[C@@](CC)(O)C3CCOCC3)(N1[C@H](C4=CC=C(Cl)C=C4)[C@H](C)C(O)=O)C5=CC=C(Cl)C=C5
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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 (79.30 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 1.5860 mL 7.9298 mL 15.8597 mL
5 mM 0.3172 mL 1.5860 mL 3.1719 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5860 mL 7.9298 mL 15.8597 mL 39.6492 mL
5 mM 0.3172 mL 1.5860 mL 3.1719 mL 7.9298 mL
10 mM 0.1586 mL 0.7930 mL 1.5860 mL 3.9649 mL
15 mM 0.1057 mL 0.5287 mL 1.0573 mL 2.6433 mL
20 mM 0.0793 mL 0.3965 mL 0.7930 mL 1.9825 mL
25 mM 0.0634 mL 0.3172 mL 0.6344 mL 1.5860 mL
30 mM 0.0529 mL 0.2643 mL 0.5287 mL 1.3216 mL
40 mM 0.0396 mL 0.1982 mL 0.3965 mL 0.9912 mL
50 mM 0.0317 mL 0.1586 mL 0.3172 mL 0.7930 mL
60 mM 0.0264 mL 0.1322 mL 0.2643 mL 0.6608 mL
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ASTX295 Related Classifications

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.

Keywords:

ASTX2952093449-12-6ASTX 295ASTX-295MDM-2/p53MDM2p53cell death and cell cycle arrestlymphoid malignanciesInhibitorinhibitorinhibit

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