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1431697-78-7

中文名稱 2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮鹽酸鹽
英文名稱 (S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride
CAS 1431697-78-7
分子式 C23H23ClN8O
分子量 462.935
MOL 文件 1431697-78-7.mol
1431697-78-7 結(jié)構(gòu)式 1431697-78-7 結(jié)構(gòu)式

基本信息

中文別名
PI3K抑制劑(CAL-130 HYDROCHLORIDE)
2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮鹽酸鹽
英文別名
CAL-130 HCl
CAL-130 (Hydrochloride)
(S)-2-(1-((2-aMino-9H-purin-6-yl)aMino)ethyl)-5-Methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride
2-[(1S)-1-[(2-Amino-9H-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone hydrochloride (1:1)
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
形態(tài)粉末
顏色Light yellow to yellow
2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮鹽酸鹽價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-16122B2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮鹽酸鹽
CAL-130 Hydrochloride
1431697-78-72mg1773元
2024/11/08HY-16122B2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮鹽酸鹽
CAL-130 Hydrochloride
1431697-78-75mg2660元
2024/11/08HY-16122B2-[(1S)-1-[(2-氨基-9H-嘌呤-6-基)氨基]乙基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮鹽酸鹽
CAL-130 Hydrochloride
1431697-78-710mM * 1mLin DMSO2709元

常見問(wèn)題列表

生物活性
CAL-130 Hydrochloride 是一種 PI3Kδ 和 PI3Kγ 抑制劑,IC50 分別為 1.3 和 6.1 nM。
靶點(diǎn)

p110δ

1.3 nM (IC 50 )

p110γ

6.1 nM (IC 50 )

p110β

56 nM (IC 50 )

p110α

115 nM (IC 50 )

體外研究

CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains. IC 50 values of CAL-130 are 1.3 and 6.1 nM for p110δ and p110γ, respectively, as compared to 115 and 56 nM for p110α and p110β. CAL-130 does not inhibit additional intracellular signaling pathways (i.e., p38 MAPK or insulin receptor tyrosine kinase) that are critical for general cell function and survival.

體內(nèi)研究

The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 to Lck/Pten fl/fl mice with established T cell acute lymphoblastic leukemia (T-ALL). Candidate animals for survival studies are ill appearing, have a white blood cell (WBC) count above 45,000 μL -1 , evidence of blasts on peripheral smear, and a majority of circulation cells (>75%) staining double positive for Thy1.2 and Ki-67. Mice receive an oral dose (10 mg/kg) of CAL-130 every 8 hr for a period of 7 days and are then followed until moribund. Despite the limited duration of therapy, CAL-130 is highly effective in extending the median survival for treated animals to 45 days as compared 7.5 days for the control group.

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