2. PROTAC Metabolic Enzyme/Protease
  3. Molecular Glues Phosphoglycerate Dehydrogenase (PHGDH)
  4. LXH-3-71

LXH-3-71 is a PHGDH degrader. LXH-3-71 acts as a molecular glue to enhance the interaction of the PHGDH-DDB1-CRL E3 ligase complex, triggering ubiquitination and proteasomal degradation of PHGDH. LXH-3-71 regulates the stemness of colorectal cancer cells and inhibits tumor proliferation and colony formation. LXH-3-71 can be used in the research of colorectal cancer.

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

LXH-3-71

LXH-3-71 Chemical Structure

CAS No. : 2251753-65-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

LXH-3-71 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LXH-3-71 is a PHGDH degrader. LXH-3-71 acts as a molecular glue to enhance the interaction of the PHGDH-DDB1-CRL E3 ligase complex, triggering ubiquitination and proteasomal degradation of PHGDH. LXH-3-71 regulates the stemness of colorectal cancer cells and inhibits tumor proliferation and colony formation. LXH-3-71 can be used in the research of colorectal cancer[1].

Cellular Effect
Cell Line Type Value Description References
4T1 IC50
5.862 μM
Compound: 55
Cytotoxicity activity against mouse 4T1 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity activity against mouse 4T1 cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 30433783]
A-375 IC50
4.633 μM
Compound: 55
Cytotoxicity activity against human A375 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity activity against human A375 cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 30433783]
A549 IC50
12.35 μM
Compound: 55
Cytotoxicity activity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity activity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 30433783]
B16-F10 IC50
5.605 μM
Compound: 55
Cytotoxicity activity against mouse B16F10 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity activity against mouse B16F10 cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 30433783]
MDA-MB-231 IC50
8.578 μM
Compound: 55
Cytotoxicity activity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity activity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 30433783]
PANC-1 IC50
5.07 μM
Compound: 55
Cytotoxicity activity against human PANC1 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity activity against human PANC1 cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 30433783]
In Vitro

LXH-3-71 (72 h) inhibits the proliferation of HCT-15, HCT-116, LoVo, SW480, CT26 and RKO colorectal cancer cells in vitro[1].
LXH-3-71 (2.5-5 μM) inhibits colony formation of HCT-116 and SW480 colorectal cancer cells[1].
LXH-3-71 (2.5-5 μM; 3 days) reduces the tumorsphere-forming ability of HCT-116 and SW480 colorectal cancer cells in a dose-dependent manner[1].
LXH-3-71 (0.5-8 μM; 0-24 h) induces dose- and time-dependent degradation of PHGDH protein via the proteasomal pathway in HCT-116 and HCT-15 colorectal cancer cells[1].

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

LXH-3-71 Related Antibodies

Cell Viability Assay[1]

Cell Line: HCT-15, HCT-116, LoVo, SW480, CT26, RKO colorectal cancer cells
Concentration: /
Incubation Time: 72 h
Result: Had IC50 values of 3.41, 1.80, 2.57, 2.60, 1.46, 4.34 for HCT-15, HCT-116, LoVo, SW480, CT26, RKO colorectal cancer cells.
In Vivo

LXH-3-71 (1-3 mg/kg; i.p.; once daily; for 17 consecutive days) dose-dependently inhibits the growth of subcutaneous colorectal tumors in BALB/c nude mice[1].
LXH-3-71 (1-3 mg/kg; i.p.; once daily; for 28 consecutive days) significantly reduces lung metastatic burden in a BALB/c nude mouse model of colorectal cancer metastasis[1].

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

Animal Model: BALB/c nude mice (female, 6 weeks old, subcutaneous xenograft via injection of 5.0 × 106 HCT-116 cells)[1]
Dosage: 1 mg/kg; 3 mg/kg
Administration: i.p.; daily; 17 days
Result: Inhibited tumor growth in a dose-dependent manner.
Significantly reduced tumor weight compared to vehicle control.
Significantly reduced Ki67-positive cell numbers in tumor tissue.
Conspicuously downregulated PHGDH protein levels in tumor tissue.
Caused no significant systemic toxicity in spleen, liver, kidney, or lung tissues.
Induced minimal body weight changes, indicating good tolerability.
Molecular Weight

657.92

Formula

C41H59N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=C1C[C@]2([C@@](C(C)(C)C1=O)([H])CC[C@]3(C)[C@]2([H])CC=C4[C@]5([H])CC(C)(CC[C@@]5(CC[C@]43C)C(NCCNC(NC6=CC=C(C=C6)OC)=O)=O)C)C
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 : 100 mg/mL (151.99 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 1.5199 mL 7.5997 mL 15.1994 mL
5 mM 0.3040 mL 1.5199 mL 3.0399 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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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)

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).
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. 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 1.5199 mL 7.5997 mL 15.1994 mL 37.9985 mL
5 mM 0.3040 mL 1.5199 mL 3.0399 mL 7.5997 mL
10 mM 0.1520 mL 0.7600 mL 1.5199 mL 3.7999 mL
15 mM 0.1013 mL 0.5066 mL 1.0133 mL 2.5332 mL
20 mM 0.0760 mL 0.3800 mL 0.7600 mL 1.8999 mL
25 mM 0.0608 mL 0.3040 mL 0.6080 mL 1.5199 mL
30 mM 0.0507 mL 0.2533 mL 0.5066 mL 1.2666 mL
40 mM 0.0380 mL 0.1900 mL 0.3800 mL 0.9500 mL
50 mM 0.0304 mL 0.1520 mL 0.3040 mL 0.7600 mL
60 mM 0.0253 mL 0.1267 mL 0.2533 mL 0.6333 mL
80 mM 0.0190 mL 0.0950 mL 0.1900 mL 0.4750 mL
100 mM 0.0152 mL 0.0760 mL 0.1520 mL 0.3800 mL
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LXH-3-71 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:

LXH-3-712251753-65-6Molecular GluesPhosphoglycerate Dehydrogenase (PHGDH)SW480DDB1-CRL E3 ligaseHCT-15CT26CD133+CD44+ HCT-116 colorectal cancer stem cellscolorectal cancer3-phosphoglycerate dehydrogenaseHCT-116LoVoPHGDHInhibitorinhibitorinhibit

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