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CAL-101,≥98%
【英文同義名】:CAL-101, CAL 101, CAL101,Idelalisib, GS-1101, GS 1101, CHEMBL2216870.
【中文同義名】:CAL-101
訂購(gòu)信息:(*,常備現(xiàn)貨)
品 牌 | 產(chǎn)品名稱 | 產(chǎn)品貨號(hào) | 規(guī) 格 | 目錄價(jià)(元) |
Gene Operation | CAL-101 | IPA1103-0005MG | 5 mg | ¥549.00 |
IPA1103-0010MG | 10 mg | ¥979.00 | ||
IPA1103-0050MG | 50mg | ¥3,629.00 |
產(chǎn)品描述
CAL-101是一種可用于口服的PI3K特異性抑制劑,主要作用靶點(diǎn)為p110δ (IC50:2.5 nM)。CAL-101作用于p110δ比作用于p110α/β/γ選擇性高40到300倍,比作用于C2β, hVPS34, DNA-PK和mTOR的選擇性則高400到4000倍。CAL-101通過(guò)抑制第二信使PIP3的產(chǎn)生,阻斷了PI3K信號(hào)通路的激活,從而誘導(dǎo)腫瘤細(xì)胞的凋亡[1]。與正常B細(xì)胞相比,CAL-101更傾向與在慢性淋巴細(xì)胞性白血?。?/span>CLL)中誘導(dǎo)產(chǎn)生細(xì)胞毒性。此外,CAL-101還能抑制炎癥性細(xì)胞因子的產(chǎn)生,例如IL-6, IL-10, TNF-α, and IFN-γ,或者激活誘導(dǎo)的細(xì)胞因子,例如CD40L。CAL-101還會(huì)拮抗CD40L介導(dǎo)的的CLL細(xì)胞存活 [2]。目前,CAL-101在CLL和慢性非霍奇金淋巴瘤(NHL)的治療中已經(jīng)處于臨床二期研究階段[3]。
靶點(diǎn)
Targets | p110δ |
IC50 | 2.5 nM |
化學(xué)特性
Cas No.: 870281-82-6 | M. Wt.: 415.42 |
Formula: C22H18FN7O | Purity: ≥98% |
Synonym: CAL-101, Idelalisib, 870281-82-6, GS-1101, CAL101, CHEMBL2216870, CAL-101, CAL101 | |
Chemical Name: (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H) -one | |
Appearance: | |
Solubility: Soluble in DMSO (25 mg/ml) | |
Storage:Store powder at -20 ºC for the stability of two years. |
結(jié)構(gòu)式
Reference
[1] Lannutti BJ,et al. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 117(2):591-4(2011).
[2] Herman SE, et al. The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood. 116(12):
2078-88(2010).
[3] Castillo JJ, et al. CAL-101: a phosphatidylinositol-3-kinase p110-delta inhibitor for the treatment of lymphoid malignancies. Expert Opin Investig Drugs. 21(1):15-22(2012).