TG 100572 Hydrochloride
产品名称:TG 100572 Hydrochloride
产品描述:
产品描述 | TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively). |
靶点活性 | PDGFRβ:13 nM, FGFR1:2 nM, FGFR2:16 nM, VEGFR1:2 nM, VEGFR2:7 nM |
体外活性 | apoptosis in rapidly proliferating, but not quiescent, endothelial cell cultures induced by TG 100572[1]. TG 100572 is shown to inhibit hRMVEC cell proliferation(IC50 of 610±72 nM). TG 100572 has the therapeutic potential to inhibit VEGF function in ocular endothelial cells, a contributing factor to pathological angiogenesis in diseases such as AMD and PDR[2]. |
体内活性 | Systemic delivery of TG 100572 in a murine model of laser-induced choroidal neovascularization (CNV) causes significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity[1]. TG 100572(23.4 μM) is reached in 30 min (Tmax)=0.5 h) in the choroid and the sclera. However, the levels of TG 100572 in the retina are relatively low. The half-life of TG 100572 in ocular tissues is very short; hence, TG 100572 is administered topically minimum t.i.d. to maintain appropriate drug levels in the eye. The maximum concentration one can achieve in formulations using TG 100572 is 0.7% w/v[2]. |
分子量 | 512.43 |
分子式 | C26H27Cl2N5O2 |
CAS No. | 867331-64-4 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 20 mg/mL (39.03 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发,涵盖生物科技、化学品、中间体和化工材料等领域。
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