IP2

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

IP2 

IP2 是一种免疫调节剂。IP2 增加癌细胞中 PTP 衍生的抗原呈递。IP2 对癌细胞无细胞毒性。IP2 在小鼠体内诱导肿瘤生长缺陷。

IP2

IP2 Chemical Structure

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生物活性

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[1].

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MCF-7, A549, HCT116, K562, MCA205, B16F10, K562R, HUVEC cells
Concentration: 10 µM
Incubation Time: 72 h
Result: Showed non-cytotoxic for cancer cells.

体内研究
(In Vivo)

IP2 (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) shows a high bioavailability in mice[1].
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

Male C57BL/6J mice and male beagle dog; 0.711 mg/kg for i.p. for mice; 9.103 mg/kg for i.v. for mice; 26.76 mg/kg for i.v. for dog[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J mice and male beagle dog[1]
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
Administration: I.p. or i.v.
Result: Exhibited a high bioavailability in mice and a very low clearance in dogs and a moderate half-life of elimination.
Animal Model: Female C57BL/6 mice[1]
Dosage: 50, 100, 250, 500 mg/kg
Administration: I.p.
Result: Showed very well toleration in C57BL/6 mice.
Animal Model: C57BL/6 mice[1]
Dosage: 5 mg/kg
Administration: Intratumor injection; three times per week for 2 weeks
Result: Shows a 50% decreased in MCA205 WT fibrosarcoma growth at killing.

分子量

830.40

Formula

C32H20Na4O17P2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Letribot B,et al. Biological Investigation of a Water-Soluble Isoginkgetin-Phosphate Analogue, Targeting the Spliceosome with In Vivo Antitumor Activity. J Med Chem. 2022; 65(6):4633-4648.

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