IP2
IP2 is an immunomodulatory agent. IP2 increases PTP (Pioneer Translation Product)-derived antigen presentation in cancer cells. IP2 shows non-cytotoxic for cancer cells. IP2 induces tumor growth defects in mouse.
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- No. CAS: 2247640-44-2
- Fòrmula: C32H20Na4O16P2
- Peso molecular:814.40
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
IP2 (35 μM) shows immunomodulatory activity in murine MCA205 fibrosarcoma cells[1].
IP2 (35 μM) increases in the intron-derived SL8 antigen presentation[1].
IP2 (10 μM; 72 h) shows non-cytotoxic for cancer cells[1].
IP2 (10 μM) shows selectivity against three G-protein coupled receptor ADRB1 (35%), HRH2 (40%), and OPRD1 (53%), and inhibits the three enzymes of COX1 (52.8%), PDE3A (84.8%), and PDE4D2 (87.2%)[1].
IP2 (10 μM) dose not induce immunogenic cell death hallmarks in human osteosarcoma U2OS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, A549, HCT116, K562, MCA205, B16F10, K562R, HUVEC cells
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Concentration:10 µM
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Incubation Time:72 h
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Result:Showed non-cytotoxic for cancer cells.
In Vivo
IP2 (50, 100, 250, 500 mg/kg; i.p.) shows very well toleration in C57BL/6 mice[1].
IP2 (2.5 mg/kg; i.v.) induces tumor growth defects in C57BL/6 mice[1].
IP2 (5 mg/kg; intratumor injection; three times per week for 2 weeks) induces tumor growth defects in C57BL/6 mice[1].
Pharmacokinetic Parameters of IP2 in Male C57BL/6J mice and male beagle dog[1].
| Dose (mg/kg) | Cmax (ng/mL) | Tmax (h) | T1/2 (h) | CL (mL/min/kg) | F % | MRT0-t (h) | AUCtot (ng/mL·h) | AUCextra (%) | |
| ip mice | 9.103 | 2078 | 0.0833 | 0.8 | 154 | 86 | 0.7 | 982.3 | 1.3 |
| iv mice | 0.711 | 322.7 | 0.0833 | 1.1 | 133 | 0.9 | 88.8 | 15.2 | |
| iv dog | 26.76 | 272 (μg/mL) | 0.0833 | 3.8 | 0.69 | 3.8 | 654.7 (μg/mL·h) | 0.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice and male beagle dog[1]
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Dosage:0.711 mg/kg for i.p. for mice; 9.103 mg/kg for i.v. for nice; 26.76 mg/kg for i.v. for dog
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Administration:I.p. or i.v.
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Result:Exhibited a high bioavailability in mice and a very low clearance in dogs and a moderate half-life of elimination.
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Animal Model:Female C57BL/6 mice[1]
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Dosage:50, 100, 250, 500 mg/kg
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Administration:I.p.
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Result:Showed very well toleration in C57BL/6 mice.
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Animal Model:C57BL/6 mice[1]
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Dosage:5 mg/kg
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Administration:Intratumor injection; three times per week for 2 weeks
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Result:Shows a 50% decreased in MCA205 WT fibrosarcoma growth at killing.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2247640-44-2
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Peso molecular 814.40
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Fòrmula C32H20Na4O16P2
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SMILES
OC1=C2C(C=C(OC2=CC(OP(O[Na])(O[Na])=O)=C1)C3=CC=C(C(C4=C(C5=C(C=C4OP(O[Na])(O[Na])=O)O)OC(C6=CC=C(C=C6)OC)=CC5=O)=C3)OC)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IP2 Related Classifications
HY-144655 Related Classifications
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