IHMT-15137 (3 μM; 24-168 h) has a synergistic effect with cisplatin (5-30 μM), which can reduce the cell viability of small cell lung cancer (SCLC) patient-derived cells C23084 and LUC22009, induce S phase cell cycle arrest, inhibit cell proliferation, promote cell apoptosis, increase DNA damage, and disrupt the BMX-ERK1/2-Cyclin D1-E2F1 signaling pathway [1]. IHMT-15137 can enhance the cytotoxic and antiproliferative effects of cisplatin combined with etoposide chemotherapy on SCLC patient-derived cells C23084 and LUC22009 [1].

IHMT-15137 (100 mg/kg; intraperitoneal injection) combined with cisplatin and etoposide inhibited 60.1% of tumor growth in H69AR small cell lung cancer xenografts, enhanced apoptosis, and inhibited cell proliferation without significant toxicity [1]. IHMT-15137 (100 mg/kg; intraperitoneal injection) combined with cisplatin and etoposide inhibited 69.0% of tumor growth in H446DDPR small cell lung cancer xenografts, enhanced apoptosis, and inhibited cell proliferation without significant toxicity [1]. IHMT-15137 (100 mg/kg; intraperitoneal injection) combined with cisplatin and etoposide inhibited 59.8% of tumor growth in small cell lung cancer patient-derived xenografts, enhanced apoptosis, and inhibited cell proliferation without significant toxicity [1].

Cell cycle analysis [1]
Cell Types: SCLC patient-derived cells C23084 and LUC22009
Tested Concentrations: 3 μM; 3 μM plus 5 μM cisplatin
Incubation Duration: 48 hours
Experimental Results: Induced S phase cell cycle arrest.

Animal/Disease Models:NCG mice (female, 6 weeks old, xenograft model with subcutaneous implantation of drug-resistant H69AR cells) [1]
Doses: 100 mg/kg; 100 mg/kg plus 2 mg/kg cisplatin plus 16 mg/kg etoposide
Route of Administration: Intraperitoneal injection
Experimental Results: Tumor growth inhibition rate (TGI) reached 60.1%. Compared with the vector control group (2.46 g), the final mean tumor weight was reduced to 0.96 g. It inhibited the increase in p-BMX (Tyr566), p-ERK1/2 (Thr202/Tyr204), cyclin D1, p-E2F1 (Ser332) and p-E2F1 (Ser337) levels in chemotherapy-induced tumor tissue. Compared with monotherapy, tumor cell apoptosis (TUNEL-positive cells) increased. Compared with monotherapy, tumor cell proliferation (Ki-67-positive cells) decreased. No significant weight loss was observed.

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Animal/Disease Models:NCG mice (female, 6 weeks old, xenograft model with subcutaneous implantation of drug-resistant H446DDPR cells) [1]
Doses: 100 mg/kg; 100 mg/kg plus 2 mg/kg cisplatin plus 16 mg/kg etoposide.
Route of Administration: Intraperitoneal injection.
Experimental Results: Tumor growth inhibition rate (TGI) reached 69.0%. Compared with the vector control group (2.52 g), the final mean tumor weight was reduced to 0.78 g. It inhibited the increase in p-BMX (Tyr566), p-ERK1/2 (Thr202/Tyr204), cyclin D1, p-E2F1 (Ser332) and p-E2F1 (Ser337) levels in chemotherapy-induced tumor tissue. Compared with monotherapy, tumor cell apoptosis (TUNEL-positive cells) increased. Compared with monotherapy, tumor cell proliferation (Ki-67-positive cells) decreased. No significant weight loss was observed.

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Animal/Disease Models:NCG mice (female, 6 weeks old, patient-derived xenograft model with subcutaneous implantation of PDC C23084 cells) [1]
Doses: 100 mg/kg; 100 mg/kg plus 2 mg/kg cisplatin plus 16 mg/kg etoposide
Route of Administration: Intraperitoneal injection
Experimental Results: Tumor growth inhibition rate (TGI) reached 59.8%. The final mean tumor weight was reduced to 0.39 g compared with the vector control group (0.97 g). It inhibited the increase in p-BMX (Tyr566), p-ERK1/2 (Thr202/Tyr204), Cyclin D1, p-E2F1 (Ser332) and p-E2F1 (Ser337) levels in chemotherapy-induced tumor tissue. Elevated levels of cleaved PARP and cleaved caspase-3 (apoptotic markers). Increased tumor cell apoptosis (TUNEL-positive cells) compared to monotherapy. Decreased tumor cell proliferation (Ki-67-positive cells) compared to monotherapy. No significant weight loss was observed.

[1]. BMX inhibition overcomes small cell lung cancer chemoresistance by stabilizing E2F1 via ERK1/2-Cyclin D1/CDK4/6 axis. Signal Transduct Target Ther. 2026;11(1):125. Published 2026 Apr 8.

C21H21F3N6O2

446.43

Typically exists as solids at room temperature

FC(F)(F)C1=CC=C(NC(C2=NNC=C2NC(CC3CN(C(C=C)=O)CCC3)=O)=N4)C4=C1

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)