2. Metabolic Enzyme/Protease
  3. Phosphoglycerate Dehydrogenase (PHGDH)
  4. PHGDH-IN-3

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer.

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

PHGDH-IN-3 Chemical Structure

PHGDH-IN-3 Chemical Structure

CAS No. : 2893778-31-7

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1 mg USD 120 In-stock
5 mg USD 290 In-stock
10 mg USD 430 In-stock
25 mg USD 690 In-stock
50 mg USD 920 In-stock
100 mg USD 1250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PHGDH-IN-3 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer[1].

IC50 & Target

IC50: 2.8 μM (PHGDH)[1].
Kd: 2.33 μM (PHGDH)[1]
In Vitro

PHGDH-IN-3 (compound D8) has good enzymatic inhibitory activity with an IC50 value of 2.8 μM[1].
PHGDH-IN-3 has high binding affinity for the PHGDH protein with a Kd value of 2.33 μM[1].
PHGDH-IN-3 has sensitivity to the cell lines with the PHGDH gene amplification or overexpression[1].
PHGDH-IN-3 can restrict the de novo serine synthesis from glucose within MDA-MB-468 cells[1].

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

PHGDH-IN-3 Related Antibodies
In Vivo

PHGDH-IN-3 (compound D8) (p.o., i.v.; 1, 3 mg/kg) exhibits excellent in vivo pharmacokinetic properties[1].
PHGDH-IN-3 (i.p.; 12.5, 25, 50 mg/kg; once daily for consecutive 31 days) exertes evident antitumor efficacy in the PC9 xenograft mouse model[1].

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

Animal Model: ICR mice[1]
Dosage: 1, 3 mg/kg
Administration: Oral (p.o.) and intravenous (i.v.) administration
Result:
PK parameters i.v. (1 mg/kg) p.o. (3 mg/kg)
AUC (h•ng/mL) 38,358 ± 14,768 94,386 ± 23,416
T1/2(h) 4.94 ± 0.38 4.74 ± 0.30
Tmax (h) 3.33 ± 1.15
CL_obs(mL/min/kg) 0.48 ± 0.23
Cmax(ng/mL) 8842 ± 1755
F (%) 82.0
Animal Model: Balb/c nude mice[1]
Dosage: 12.5, 25, 50 mg/kg
Administration: Intraperitoneal (i.p.); once daily for consecutive 31 days
Result: Exhibited an in vivo anti-tumor effect and significantly delayed the tumor growth.
Significantly abated the tumor weights of mice at 25 mg/ kg.
Molecular Weight

495.55

Formula

C24H18FN3O4S2
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

CC(C1=CC=CC(NS(=O)(C2=CC=C(C=C2)C(NC3=NC(C4=CC=CC(F)=C4)=CS3)=O)=O)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (201.80 mM; ultrasonic and warming and heat to 70°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 2.0180 mL 10.0898 mL 20.1796 mL
5 mM 0.4036 mL 2.0180 mL 4.0359 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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)

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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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (10.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (protect from 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
DMSO 1 mM 2.0180 mL 10.0898 mL 20.1796 mL 50.4490 mL
5 mM 0.4036 mL 2.0180 mL 4.0359 mL 10.0898 mL
10 mM 0.2018 mL 1.0090 mL 2.0180 mL 5.0449 mL
15 mM 0.1345 mL 0.6727 mL 1.3453 mL 3.3633 mL
20 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5224 mL
25 mM 0.0807 mL 0.4036 mL 0.8072 mL 2.0180 mL
30 mM 0.0673 mL 0.3363 mL 0.6727 mL 1.6816 mL
40 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.2612 mL
50 mM 0.0404 mL 0.2018 mL 0.4036 mL 1.0090 mL
60 mM 0.0336 mL 0.1682 mL 0.3363 mL 0.8408 mL
80 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6306 mL
100 mM 0.0202 mL 0.1009 mL 0.2018 mL 0.5045 mL
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PHGDH-IN-3 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:

PHGDH-IN-32893778-31-7Phosphoglycerate Dehydrogenase (PHGDH)oralphosphoglycerate dehydrogenase (PHGDH)MDA-MB-468cancerInhibitorinhibitorinhibit

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