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XL228 Sale

(Synonyms: N4-(5-环丙基-1H-吡唑-3-基)-N2-[[3-异丙基-5-异恶唑基]甲基]-6-(4-甲基-1-哌嗪基)-2,4-嘧啶二胺,XL-228;XL 228) 目录号 : GC13102

A tyrosine kinase inhibitor

XL228 Chemical Structure

Cas No.:898280-07-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO) 待询 待询
5mg
¥1,088.00
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10mg
¥1,507.00
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25mg 待询 待询
50mg
¥4,185.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

XL228, a tyrosine kinase inhibitor, is involved in binding to and inhibiting the activities of multiple tyrosine kinases, such as the insulin-like growth factor 1 receptor (IGF1R), Src tyrosine kinase, and Bcr-Abl tyrosine kinase. Blockade of these kinases may result in the inhibition of tumor angiogenesis, cell proliferation, and metastasis [1]. XL228 is a multitargeted protein kinase inhibitor targeting IGF1R, the aurora kinases, IGF-1R, cSrc, BCR/Abl and SRC kinases [2].

In vitro: XL228(5-100 nM) reduced cell survival by 10-70% in a dose and time dependent manner and inhibited migration and invasion of two tumors with high propensity to metastasize, FaDu and H460. Treatment with 50 and 100 nM XL228 abolished the ability of H460, A549 and FaDu cells to form colony. At 10 nM, XL228 significantly increased the radiosensitivity of H460, A549 and FaDu cells by enhancement factors (EF, at the survival fraction of 0.5) of 1.52, 1.31 and 1.67 respectively. But, In HN-5 cells, sensitization occurred only at 100 nM (EF = 2.27). In HN-5 cells, XL228 (100 nM)incubation induced accumulation of cells at the radiation sensitive G2/M phase of the cell cycle and induced apoptosis in 32% of cells [2].

Clinical trial: In a phase I study in patients with solid tumors or hematologic malignancies, XL228 showed a manageable toxicity profile and biological activity through decrease in target pathway and alternations in tumor nuclei [3].

References:
[1] Smith D C, Britten C, Garon E B.  A phase I study of XL228, a multitargeted protein kinase inhibitor, in patients with solid tumors or multiple myeloma[J]. J ClinOncol, 2010, 28(15s suppl: abstr 3105).
[2] Matsumoto F, Molkentine D, Clary D O, et al.  A multi-kinase inhibitor, XL228, enhanced human cancer cell radiosensitivity and suppressed cell invasion and migration[J]. Cancer Research, 2011, 71(8 Supplement): 2487-2487.
[3] Smith D C, Britten C, Clary D O, et al.  A phase I study of XL228, a potent IGF1R/AURORA/SRC inhibitor, in patients with solid tumors or hematologic malignancies[J]. J ClinOncol, 2009, 27(15 suppl): 149s.

Chemical Properties

Cas No. 898280-07-4 SDF
别名 N4-(5-环丙基-1H-吡唑-3-基)-N2-[[3-异丙基-5-异恶唑基]甲基]-6-(4-甲基-1-哌嗪基)-2,4-嘧啶二胺,XL-228;XL 228
化学名 4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-N-[(3-propan-2-yl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine
Canonical SMILES CC(C)C1=NOC(=C1)CNC2=NC(=CC(=N2)NC3=NNC(=C3)C4CC4)N5CCN(CC5)C
分子式 C22H31N9O 分子量 437.54
溶解度 ≥ 21.9 mg/mL in DMSO, ≥ 27.6 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mM 2.2855 mL 11.4275 mL 22.8551 mL
5 mM 0.4571 mL 2.2855 mL 4.571 mL
10 mM 0.2286 mL 1.1428 mL 2.2855 mL
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