| ln Vitro |
HM-279 exhibits excellent kinase selectivity, inhibiting only 9 kinases: AurA, BUB1/BUB3, FLT4, KDR, NuakK1, PDGFRα, PDGFRβ, QIK, and MST1[1]. HM-279 showed weak antiproliferative activity against CT26 cells (IC50 = 15 μM). HM-279 (1.5 h; 1–300 nM) strongly inhibited phosphorylation of Smad3 in A549 cells (IC50 = 21.6 nM)[1].
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| ln Vivo |
HM-279 (30 mg/kg; orally; 5 days on, 2 days off; for 20 days) induces antitumor activity by modulating antitumor immunity rather than directly killing cancer cells in female BALB/cCrSlc mice subcutaneously inoculated with CT26.WT cells[1]. HM-279 (30 mg/kg; orally; 5 days on, 2 days off; for 15 days) lost its antitumor activity in female BALB/cSlc-nu/nu mice and female BALB/cCrSlc mice treated with antiCD8 antibody (5 mg/kg; intraperitoneally; twice a week), confirming that CD8+ T cells are involved in the antitumor immune response induced by HM-279[1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: A549 cells Tested Concentrations: 1 nM; 3 nM; 10 nM; 30 nM; 100 nM; 300 nM Incubation Duration: 1.5 hours Experimental Results: The 300 nM group completely inhibited the phosphorylation of Smad3. |
| Animal Protocol |
Animal/Disease Models:CT26.WT cells (1 × 10⁶ cells) were subcutaneously inoculated into the flank of 7-week-old female BALB/c Slc-nu/nu mice to establish a xenograft model [1].
Doses: 30 mg/kg Route of Administration: Oral administration; 5 days on, 2 days off; 15 days in total Experimental Results: No antitumor activity was observed. Animal/Disease Models:Female BALB/cCrSlc mice (7 weeks old) were treated with either anti-CD8 antibody (5 mg/kg; intraperitoneal injection; twice weekly) or isotype control antibody (5 mg/kg; intraperitoneal injection; twice weekly) to establish a CD8 depletion model. CT26.WT cells (1 × 10⁶ cells)[1] were then subcutaneously inoculated into the lateral abdomen of the mice. Doses: 30 mg/kg Route of Administration: Oral administration; 5 days on, 2 days off; for 15 days Experimental Experimental Results: No antitumor activity was observed in either the isotype control combined treatment group or the anti-CD8 combined treatment group. Animal/Disease Models:CT26.WT cells (1 × 10⁶ cells) were subcutaneously inoculated into the flank of 7-week-old female BALB/cCrSlc mice to establish a homology model [1]. Doses: 30 mg/kg; 30 mg/kg combined with anti-PD-1 antibody (10 mg/kg; intraperitoneal injection; twice weekly) Route of Administration: Oral; 5 days on/2 days off; 20 days Experimental Results: Oral administration showed partial antitumor activity, with a tumor growth inhibition rate (TGI) of 60%, and did not cause weight loss. When used in combination with anti-PD-1 antibody, the TGI was 89%. |
| References |
| CAS # |
3039954-64-5
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| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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