| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SIBP-03 (10⁻⁴-10⁴ ng/mL) binds specifically and strongly to recombinant human HER3 protein, but does not bind to recombinant human EGFR, HER2 or HER4 protein [1]. SIBP-03 binds to HER3 on the surface of MC38/HER3 cells that overexpress HER3, but does not bind to HER3-negative MC38 cells [1]. SIBP-03 (0.01-10 μg/mL; after pre-incubating cells stimulated by NRG1 for 2 hours, FaDu/BT-474 cells were treated with SIBP-03 for 24 hours) effectively inhibited ligand-independent and ligand-dependent HER3 activation in FaDu, BT-474 and NRG1-stimulated MCF7 and BT-474 cells, as well as downstream PI3K/AKT signaling pathways [1]. SIBP-03 (0.01-100 μg/mL; 120 h) showed weak antiproliferative effects against FaDu, A549, BT-474, SK-BR-3, and NCI-N87 cells, but effectively inhibited the proliferation of NRG1-stimulated MCF7 cells, with an inhibition rate of 74.8% at a concentration of 100 μg/mL [1]. SIBP-03 (10-100 μg/mL; 1 h) did not induce complement-dependent cytotoxicity in FaDu cells or HER3-overexpressing MC38/HER3 cells at concentrations of 10 and 100 μg/mL [1]. SIBP-03 (10-100 μg/mL; 5 h) could induce ADCC activity in HER3-overexpressing MC38/HER3 cells, but could not induce such activity in BT-474 cells at concentrations of 10 and 100 μg/mL [1]. SIBP-03 (10-100 μg/mL; 5 h) can induce antibody-dependent phagocytic activity in human breast cancer BT-474 cells and HER3-overexpressing MC38/HER3 cells at concentrations of 10 μg/mL and 100 μg/mL [1]. SIBP-03 (30 μg/mL; 144 h) can synergistically enhance the antiproliferative activity of DS-8201 in SK-BR-3 and MDA-MB-453 cells [2].
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| ln Vivo |
SIBP-03 (0.2-2 mg/kg; intravenous injection) showed potent antitumor activity in the FaDu xenograft mouse model, with a tumor growth inhibition rate (TGI) of 116.3% at a dose of 2 mg/kg, and sustained inhibition of the HER3/AKT signaling pathway for up to 168 hours after a single intravenous injection [1]. SIBP-03 (6 mg/kg; intravenous injection) showed significant antitumor activity in the A549 xenograft mouse model, with a tumor growth inhibition rate (TGI) of 57.5% at a dose of 6 mg/kg [1]. SIBP-03 (20 mg/kg; intravenous injection) showed significant antitumor activity in the NCI-N87 xenograft mouse model, with a tumor growth inhibition rate (TGI) of 50.8% at a dose of 20 mg/kg [1]. A single dose of SIBP-03 (0.6 mg/kg; iv) resulted in a TGI of 96% in mice carrying FaDu xenografts, while combined treatment with cetuximab resulted in a TGI of 152% and tumor regression in 66.7% of the mice [1].
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| References |
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
[SIBP-03]
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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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