1. Metabolic Enzyme/Protease
  2. Endogenous Metabolite
  3. SAICAR

SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions.

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SAICAR Chemical Structure

SAICAR Chemical Structure

CAS No. : 3031-95-6

Size Price Stock Quantity
500 μg USD 200 In-stock
1 mg USD 340 In-stock
5 mg USD 1200 In-stock
10 mg USD 1920 In-stock
25 mg USD 3840 In-stock
50 mg USD 6140 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of SAICAR:

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Description

SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions[1][2].

IC50 & Target[1]

Human Endogenous Metabolite

 

In Vitro

SAICAR accumulation induces nuclear localization of PKM2. PKM2-SAICAR phosphorylates and activates Erk1/2, which in turn sensitizes PKM2 for SAICAR binding through phosphorylation. Additionally, PKM2-SAICAR was necessary to induce sustained Erk1/2 activation and mitogen-induced cell proliferation. SAICAR-PKM2 interaction is necessary and sufficient to induce H3 T11 and Erk1/2 phosphorylation[2].
Upon glucose starvation, cellular SAICAR concentration increases in an oscillatory manner and stimulates PKM2 activity in cancer cells. The SAICAR-PKM2 interaction also promotes cancer cell survival in glucose-limited conditions. In glucose-limited conditions, cells with higher SAICAR concentrations (adsl-kd cells or cells overexpressing PAICS) survive better while paics-kd cells died earlier than control-kd cells. SAICAR promotes cancer cell survival in glucose-limited conditions[3].

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

Molecular Weight

454.28

Formula

C13H19N4O12P

CAS No.
Appearance

Solid

Color

Purple to purplish red

SMILES

O=C(O)C[C@@H](C(O)=O)NC(C1=C(N)N([C@H]2[C@@H]([C@@H]([C@@H](COP(O)(O)=O)O2)O)O)C=N1)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 220 mg/mL (484.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (220.13 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2013 mL 11.0064 mL 22.0129 mL
5 mM 0.4403 mL 2.2013 mL 4.4026 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 5.5 mg/mL (12.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 5.5 mg/mL (12.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
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 (sealed storage, away from moisture and light). 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
H2O / DMSO 1 mM 2.2013 mL 11.0064 mL 22.0129 mL 55.0321 mL
5 mM 0.4403 mL 2.2013 mL 4.4026 mL 11.0064 mL
10 mM 0.2201 mL 1.1006 mL 2.2013 mL 5.5032 mL
15 mM 0.1468 mL 0.7338 mL 1.4675 mL 3.6688 mL
20 mM 0.1101 mL 0.5503 mL 1.1006 mL 2.7516 mL
25 mM 0.0881 mL 0.4403 mL 0.8805 mL 2.2013 mL
30 mM 0.0734 mL 0.3669 mL 0.7338 mL 1.8344 mL
40 mM 0.0550 mL 0.2752 mL 0.5503 mL 1.3758 mL
50 mM 0.0440 mL 0.2201 mL 0.4403 mL 1.1006 mL
60 mM 0.0367 mL 0.1834 mL 0.3669 mL 0.9172 mL
80 mM 0.0275 mL 0.1376 mL 0.2752 mL 0.6879 mL
100 mM 0.0220 mL 0.1101 mL 0.2201 mL 0.5503 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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SAICAR 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.

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SAICAR
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