CAL-101
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CAL-101 ??
- ???
- 250-252oC
- ?? ?
- 733.4±70.0 °C(Predicted)
- ??
- 1.47
- ?? ??
- -20°C
- ???
- DMSO? ???(>25 mg/ml)
- ??? ??
- ?? ??.
- ?? ?? (pKa)
- 10.00±0.10(Predicted)
- ??
- ???
- ???
- ??? ?? ?????? 1? ?? ??????. DMSO? ???? -20°C?? ?? 2?? ?? ??? ? ????.
- InChIKey
- IFSDAJWBUCMOAH-HNNXBMFYSA-N
- SMILES
- N1C2=C(C(F)=CC=C2)C(=O)N(C2=CC=CC=C2)C=1[C@@H](NC1=C2C(=NC=N1)NC=N2)CC
??
- ?? ? ?? ??
- ?? ? ???? ?? (GHS)
| ????? | V | ||
|---|---|---|---|
| HS ?? | 29399990 | ||
| ?? ?? ??? | 870281-82-6(Hazardous Substances Data) |
| ????(GHS): |
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| ?? ?: | Danger | ||||||||||||||
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CAL-101 C??? ??, ??, ??
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CAL-101 is a PI3K/mTOR pathway inhibitor used in the treatment of myeloid leukemia through sensitizing the cells to combatting drugs. Potent PI3K-p110-delta inhibitor.??
ChEBI: A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indol nt non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia.in vitro
CAL-101 (Idelalisib) is a highly selective and potent p110δ inhibitor (EC50=8 nM). Greater selectivity (400- to 4000-fold) is seen against related kinases C2β, hVPS34, DNA-PK, and mTOR, whereas no activity is observed against a panel of 402 diverse kinases at 10 μM. CAL-101 reduces PDGF-induced pAkt by only 25% at 10 μM. Idelalisib (CAL-101) inhibits LPA-induced pAkt with an EC50 of 1.9 μM. Idelalisib (CAL-101) blocks Fc?RI p110δ-mediated CD63 expression with an EC50 of 8 nM, whereas formyl-methionyl-leucyl-phenylalanine activation of p110γ is inhibited with an EC50 of 3 μM. Thus, CAL-101 has 240- to 2500-fold selectivity in cell-based assays for p110δ over the other class I PI3K isoforms. CAL-101Idelalisib (CAL-101)-induced apoptosis of chronic lymphocytic leukemia (CLL) cells is significant compared with vehicle treatment alone (P<0.001). Idelalisib (CAL-101) induces selective cytotoxicity in CLL cells independent of IgVH mutational status or interphase cytogenetics.CAL-101 ?? ?? ? ???
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CAL-101 ?? ??
???( 301)?? ??
| ??? | ?? | ??? | ?? | ?? ? | ?? |
|---|---|---|---|---|---|
| Changzhou Rokechem Technology Co., Ltd. | 18758118018 |
sales001@rokechem.com | China | 255 | 58 |
| Protheragen-ING | +16313385890 |
info@protheragen-ing.com | United States | 3868 | 58 |
| Hebei Yanxi Chemical Co., Ltd. | +8617531153977 |
allison@yan-xi.com | China | 5853 | 58 |
| Capot Chemical Co.,Ltd. | +86-（0）57185586718 +86-13336195806 |
sales@capot.com | China | 29730 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 33024 | 60 |
| Lianyungang happen teng technology co., LTD | 15950718863 |
wang666xt@163.com | CHINA | 295 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29856 | 58 |
| Zhejiang ZETian Fine Chemicals Co. LTD | +8618957127338 |
stella@zetchem.com | China | 2136 | 58 |
| Biochempartner | 0086-13720134139 |
candy@biochempartner.com | CHINA | 965 | 58 |
| Hangzhou Cyanochem Co., Ltd. | +86 17788583750 |
sales@cyanochem.com | CHINA | 281 | 58 |
CAL-101 ?? ??:
????
ARRY-334543
Dovitinib
2-Amino-6-fluorobenzoic acid
(S)-2-(1-aMinopropyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
BOC-ABU-OH
(S)-tert-butyl (1-(5-fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)propyl)carbaMate
2-Fluoro-6-nitro-N-phenylbenzamide
Everolimus
Bortezomib
BKM120 (NVP-BKM120, Buparlisib)
Pictilisib
IPI 145
Ibrutinib
Selumetinib Sulfate
CO-1686
Momelotinib
790299-79-5