Cat. No.: HY-177742

LXH-3-71

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Based on 1 Customer Validation

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.

Purity: 97.19%
CAS No.: 2251753-65-6
Formula: C₄₁H₅₉N₃O₄
Molecular Weight:657.92

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LXH-3-71 Chemical Structure

CAS No.: 2251753-65-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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.

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.

Chemical Information

CAS No. 2251753-65-6
Appearance Solid
Molecular Weight 657.92
Formula C₄₁H₅₉N₃O₄
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5199 mL

7.5997 mL

15.1994 mL

5 mM

0.3040 mL

1.5199 mL

3.0399 mL

10 mM

0.1520 mL

0.7600 mL

1.5199 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Huang Z, et al. Molecular glue triggers degradation of PHGDH by enhancing the interaction between DDB1 and PHGDH. Acta Pharm Sin B. 2024;14(9):4001-4013. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioactive Compound Library Max

Bioactive Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Colorectal Cancer Compound Library

Molecular Glue Compound Library

Metabolic Enzyme Compound Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LXH-3-71

Bioactive Compound Library Max

Bioactive Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Colorectal Cancer Compound Library

Molecular Glue Compound Library

Metabolic Enzyme Compound Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LXH-3-71 Related Classifications

HY-177742 Related Classifications