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

ASTX295 is an orally active and selective MDM2 antagonist with an IC50 of <1 nM. ASTX295 inhibits the MDM2-p53 interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer.

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

ASTX295

ASTX295 Chemical Structure

CAS No. : 2093449-12-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

ASTX295 Related Antibodies

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

ASTX295 is an orally active and selective MDM2 antagonist with an IC50 of <1 nM. ASTX295 inhibits the MDM2-p53 interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer[1][2].

In Vitro

ASTX295 (0-10000 nM; up to 72 h) reduces viability in all tested TP53WT lymphoid malignancy cell lines (DLBCL, MCL, T-cell lymphoma) with IC50 values of <1 nM to 100 nM over up to 72 h, induces p53 and p21 expression, and causes maximal cell death at 72 h (24 h in Z138 cells)[1].
ASTX295 (1 μM; 0-24 h, in combination with a p53 corrector) induces sustained upregulation of p53 signaling and DNA damage-related protein and mRNA biomarkers over a 24-hour period in BxPC3 (TP53: Y220C) cells[2].

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

ASTX295 Related Antibodies

Western Blot Analysis[2]

Cell Line: BxPC3 (TP53: Y220C)
Concentration: 1 μM (in combination with p53 corrector)
Incubation Time: 0, 2, 4, 6, 8, 24 h
Result: Sustained upregulation of p53, phospho-p53 (S15), MDM2, p21, PUMA, phospho-CHK1 (S345), and phospho-H2A.X (S139) proteins through 24 h.
In Vivo

ASTX295 (80 mg/kg; p.o.; twice weekly; 6 doses) and PC14586 significantly reduces tumor volume in male CB17 SCID mice bearing BxPC3 xenografts[2].
ASTX295 (80 mg/kg; p.o.; single dose) with PC14586 in BxPC3 tumor-bearing mice significantly increases the levels of p53 signaling pathway biomarkers (tissue p21, plasma GDF-15, p21/MDM2/GDF-15 mRNA in tumor tissue, and multiple protein biomarkers)[2].

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

Animal Model: BxPC3-tumor bearing mice[2]
Dosage: 80 mg/kg
Administration: p.o.; single dose; administered 3 hours after 100 mg/kg PC14586 p.o.
Result: Increased relative tumor p21 levels up to ~45-fold relative to vehicle control at 16 hours post-dose.
Increased human GDF-15 levels in mouse plasma up to ~3.5 ng/ml at 16 hours post-dose, relative to PC14586 alone.
Upregulated tumor p21, MDM2, and GDF-15 mRNA at 16 hours post-dose.
Sustained upregulation of p53 signalling biomarkers (including p-p53 [S15], p21, PUMA, and p-H2A.X [S139]) at 16 hours post-dose by Western blotting.
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
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 : 41.18 mg/mL (65.31 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)

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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Purity & Documentation

Purity: 99.81%

SDS (251 KB)

COA (260 KB) HNMR (329 KB) LCMS (103 KB)

Handling Instructions (2659 KB)
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/p53CaspaseApoptosispancreatic cancerTP53caspasemantle cell lymphomaInhibitorinhibitorinhibit

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