DMUP is a potent CD47-SIRPα axis inhibitor. DMUP causes apoptosis and increases macrophage phagocytosis in A549 cells. DMUP reduced the protein expression levels of CD47 and SIRPα. DMUP showed anti-tumor effects.

Physicochemical Properties

Exact Mass	761.014
CAS #	2364350-07-0
PubChem CID	171360935
Appearance	White to light yellow solid powder
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	14
Rotatable Bond Count	8
Heavy Atom Count	39
Complexity	834
Defined Atom Stereocenter Count	0
InChi Key	AZMDFXAQYFEMCT-UHFFFAOYSA-L
InChi Code	InChI=1S/2C12H10O5.2Cl.2HN.Pt/c2*1-7-4-12(15)17-10-5-8(2-3-9(7)10)16-6-11(13)14;;;;;/h2*2-5H,6H2,1H3,(H,13,14);;;2*1H;/q;;4*-1;/p-2
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro	A549, A549/DDP, PANC-1, and HepG2 cells exhibit anti-proliferative activity in response to DMUP (72 hours), with IC50 values of 0.92, 3.58, 6.29, and 1.54 µM, respectively [1]. A549 cells have their cell cycle stopped in the S phase by DMUP (5 µM, 24 hours) [1]. A549 cells undergo apoptosis when exposed to 5 µM DMUP for 48 hours [1]. The 24 hour DMUP (5 µM) treatment lowers the expression of SIRPα and CD47 [1]. In A549-GFP cells, DMUP (5 µM, 4 hours) boosts macrophage phagocytosis [1].
ln Vivo	DMUP (10 mg/kg, intravenously, every other day for 17 days) showed anti-tumor efficacy [1]. DMUP (5, 10, 20, 40 mg/kg, intravenously every two days for 18 days) demonstrated no harm in mice [1].
Cell Assay	Cell proliferation assay[1] Cell Types: A549, A549/DDP, PANC-1, HepG2 Cell Tested Concentrations: 0-64 µM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated anti-proliferative activity, the IC50 of A549 was 0.92, 3.58, 6.29, 1.54 µM, A549/DDP, PANC-1, HepG2 cells. Cell cycle analysis[1] Cell Types: A549 Cell Tested Concentrations: 5 µM Incubation Duration: 24 hrs (hours) Experimental Results: Cell cycle arrested in S phase. Apoptosis analysis[1] Cell Types: A549 Cell Tested Concentrations: 5 µM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of apoptosis. Western Blot Analysis [1] Cell Types: A549, THP-1 Cell Tested Concentrations: 5 µM Incubation Duration: 24 h Experimental Results: CD47 and SIRPα protein expression diminished.
Animal Protocol	Animal/Disease Models: ICR mice [1] Doses: 5, 10, 20, 40 mg/kg Route of Administration: intravenous (iv) (iv)injection, once every two days, 18 days Experimental Results: low toxicity, LD50 greater than 20 mg/kg. Animal/Disease Models: A549 xenograft BALB/c nude mice [1] Doses: 10 mg/kg Route of Administration: intravenous (iv) (iv)injection, every other day, 17 days Experimental Results:demonstrated anti-tumor activity.
References	[1]. Tan Y, et al. Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer. Eur J Med Chem. 2022; 229:114047.

Solubility Data

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

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 (e.g. IP/IV/IM/SC) 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). 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) 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). 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 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.  (Please use freshly prepared in vivo formulations for optimal results.)