research use only
Cat.No.S2700
| Related Targets | EGFR VEGFR JAK FGFR PDGFR HIF FLT3 HER2 FLT Bcr-Abl |
|---|---|
| Other Src Inhibitors | WH-4-023 Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 UM-164 RK 24466 eCF506 Tolimidone (MLR-1023) |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| mouse NIH3T3 cells | Function assay | 3 days | Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 86 mg/mL
(199.29 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Molecular Weight | 431.53 | Formula | C26H29N3O3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 897016-82-9 | Download SDF | Storage of Stock Solutions |
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| Synonyms | KX2-391,KX 01 | SMILES | C1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4 | ||
Read more about storage stability stock solution CAS number SMILES
| Targets/IC50/Ki |
Src (HuH7)
(Cell-free assay) 9 nM(GI50)
Src (PLC/PRF/5)
(Cell-free assay) 13 nM(GI50)
Src (Hep 3B)
(Cell-free assay) 26 nM(GI50)
Src (Hep G2)
(Cell-free assay) 60 nM(GI50)
|
|---|---|
| In vitro |
KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines. KX2-391 is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. KX2-391 is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively. |
| In vivo |
In pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis. |
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | α-SMA / Collagen 1 / Fibronectin / p-Src / Src |
|
29137389 |
(data from https://clinicaltrials.gov, updated on 2025-09-17)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT07010692 | RECRUITING | Keratinocyte Carcinoma; Basal Cell Carcinomas; Squamous Cell Carcinoma; Skin Cancer |
Bruce Robinson, MD |
2025-05-16 | PHASE1; PHASE2 |
| NCT07273656 | NOT_YET_RECRUITING | Keratosis; Actinic Keratoses |
University Hospital, Lille |
2026-11-30 | PHASE3 |
| NCT06112522 | RECRUITING | Cell Carcinoma |
Centre Hospitalier Universitaire de Nice |
2024-02-16 | PHASE2 |
| NCT05387525 | ACTIVE_NOT_RECRUITING | Keratosis, Actinic |
Almirall, S.A. |
2022-10-24 | PHASE4 |
| NCT06791525 | RECRUITING | Warts Hand |
The Skin Center Dermatology Group |
2025-05-01 | PHASE4 |
| NCT06135415 | COMPLETED | Keratosis, Actinic |
Almirall, S.A. |
2023-12-21 | PHASE3 |
Read more about Clinical Trials
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Question 1:
How to formulate it for animal trials?
Answer:
It can be dissolved in 4% DMSO/corn oil at 5 mg/ml as a homogeneous suspension for oral administration and dissolved in 4% DMSO/30% PEG 300/ddH2O at 5 mg/ml as a clear solution.