PRT062607 acetate

CAS: 1370261-98-5 F: C21H27N9O3 W: 453.50

PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction A

Contact QiTai

This product is for research use only, not for human use. We do not sell to patients.

Bioactivity	PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models[1].[2].
Invitro	PRT062607 acetate 对多种激酶也有显著活性，IC50s 分别为 81 nM (Fgr)，88 nM (MLK1)，123 nM (Yes)，139 nM (Flt3)，166 nM (PAK5)，192 nM (Lyn)，244 nM (cSRC)，249 nM (Lck)，108 nM (Pyk)，415 nM (FAK)，1.05 nM (ZAP-70)[1]。PRT062607 acetate (0.01-2 μM; 3 d) 可抑制 Ramos 细胞中 ERK(Y204)、AKT(S473) 和 SYK(Y352) 的磷酸化，以及抑制 BLNK Tyr84 磷酸化[1][2]。PRT062607 acetate (2 μM; 24 h) 在 SU-DHL6 细胞中诱导凋亡[1]。在人全血中，P505-15 可有效抑制 B 细胞抗原受体介导的 B 细胞信号传导和激活 (IC50: 0.27 和 0.28 μM) 和 Fc 受体 1 介导的嗜碱性粒细胞脱颗粒 (IC50: 0.15 μM)[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PRT062607 acetate 相关抗体: Western Blot Analysis Cell Line:
In Vivo	PRT062607 acetate 在两种啮齿动物的类风湿性关节炎模型中产生了剂量依赖性抗炎活性。PRT062607 acetate (15, 30 mg/kg; po; bid; 5 d) 在小鼠体内引起 SYK 抑制，可防止 BCR 诱导的小鼠脾脏肿大[1]。PRT062607 acetate (15 mg/kg; po; bid; 5 d) 在小鼠体内引起 SYK 抑制，可防止小鼠异种移植模型中的 Ramos 肿瘤形成[1]。PRT062607 acetate (10-20 mg/kg; po; bid) 可防止 BCR 介导的脾肿大，并在异种移植模型中显着抑制 NHL 肿瘤生长[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	1370261-98-5
Formula	C21H27N9O3
Molar Mass	453.50
Appearance	固体
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Spurgeon SE, et al. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther. 2013 Feb;344(2):378-87. [2]. Coffey G, et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012 Feb;340(2):350-9.