ChemicalBook > CAS DataBase List > CAL-101

CAL-101

Product Name
CAL-101
CAS No.
870281-82-6
Chemical Name
CAL-101
Synonyms
Idelalisib(CAL-101);-101;CS-34;GS1101;AL-101;CAL-11;CAL-101;CAL-101 1KG;CAL101,CAL-101;CAL-101, >=98%
CBNumber
CB32538915
Molecular Formula
C22H18FN7O
Formula Weight
415.42
MOL File
870281-82-6.mol
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CAL-101 Property

Melting point:
250-252oC
Boiling point:
733.4±70.0 °C(Predicted)
Density 
1.47
storage temp. 
-20°C
solubility 
Soluble in DMSO (>25 mg/ml)
form 
White solid.
pka
10.00±0.10(Predicted)
color 
White
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
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
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Safety

Safety Statements 
V
HS Code 
29399990
Hazardous Substances Data
870281-82-6(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P314Get medical advice/attention if you feel unwell.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
15279
Product name
CAL-101
Purity
≥98%
Packaging
5mg
Price
$33
Updated
2024/03/01
Cayman Chemical
Product number
15279
Product name
CAL-101
Purity
≥98%
Packaging
10mg
Price
$63
Updated
2024/03/01
Cayman Chemical
Product number
15279
Product name
CAL-101
Purity
≥98%
Packaging
25mg
Price
$107
Updated
2024/03/01
Cayman Chemical
Product number
15279
Product name
CAL-101
Purity
≥98%
Packaging
50mg
Price
$164
Updated
2024/03/01
TRC
Product number
C124800
Product name
CAL-101
Packaging
100mg
Price
$285
Updated
2021/12/16
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CAL-101 Chemical Properties,Usage,Production

Description

Idelalisib (CAS 870281-82-6) is a potent (IC50 = 2.5nM) and selective (IC50’s: PI3Ka = 820nM, PI3Kb = 565nM, PI3Kg = 89nM) PI3Kd inhibitor.1,2 Useful clinical agent for the treatment of various blood cancers. Idelalisib attenuates regulatory T cells (Treg) but not conventional T cells (Tconv) resulting in a significant increase in tumor-infiltrating antigen-specific CD8 T cells in a murine lung cancer model.3 Conversely, systemic PI3Kd inactivation antagonized anti-CTLA-4 and anti-PD-L1 treatment.4 Others have found that Idelalisib minimally influenced rituximab- and obinutuzumab-mediated Ab-dependent cellular cytotoxicity in human lymphoma cells.5

Uses

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.

Definition

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.

in vivo

A significant reduction is observed in the CD11b+Ly6G+ neutrophils from brain homogenates of bothp110δD910A/D910A mice and Idelalisib (CAL-101) (40 mg/kg, i.v.) post-treated mice.

target

p110δ

storage

Store at -20°C

References

1) Herman?et al. (2010), Phosphatidylinositol 2-kinase-d inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals; Blood?116 2078 2) Lannutti?et al. (2011), CAL-101, a p110d selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability; Blood 117 591 3) Ahmad?et al. (2017), Differential PI3Kd Signaling in CD4+ T-cell Subsets Enables Selective Targeting of T Regulatory Cells to Enhance Cancer Immunotherapy; Cancer Res. 77 1892 4) Lim?et al. (2018), Phosphoinositide 3-kinase d inhibition promotes antitumor responses but antagonizes checkpoint inhibitors; JCI Insight 3 e120626 5) Palazzo?et al.?(2018),?The PI3Kd-Selective Inhibitor Idelalisib Minimally Interferes with Immune Effector Function Mediated by Rituximab or Obinutuzumab and Significantly Augment B Cell Depletion In Vivo; J.Immunol. 200 2304

CAL-101 Preparation Products And Raw materials

Raw materials

Preparation Products

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CAL-101 Suppliers

China 251 China Hong Kong 1 India 6 Japan 1 United Kingdom 3 United States 27 Global 289
AdooQ BioScience, LLC
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marketing@targetmol.com
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View Lastest Price from CAL-101 manufacturers

HangZhou RunYan Pharma Technology Co.,LTD.
Product
CAL-101 870281-82-6
Price
US $0.00-0.00/g
Min. Order
1g
Purity
99% HPLC
Supply Ability
10000
Release date
2024-09-22
Hebei Yanxi Chemical Co., Ltd.
Product
CAL-101 870281-82-6
Price
US $0.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
20tons
Release date
2023-10-09
PUSHAN INDUSTRIAL (SHAANXI) CO.,LTD
Product
Idelalisib 870281-82-6
Price
US $0.00/kg
Min. Order
1kg
Purity
98% HPLC
Supply Ability
500 kgs
Release date
2024-05-13

870281-82-6, CAL-101Related Search:

AZD-6244 ARRY-334543 Dovitinib Volitinib 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 CO-1686 Momelotinib 790299-79-5

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  • 4(3H)-Quinazolinone, 5-fluoro-3-phenyl-2-[(1S)-1-(1H-purin-6-ylaMino)propyl]-
  • 5-Fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]quinazolin-4-one
  • 5-Fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone CAL-101 (Idelalisib, GS-1101)
  • CAL-101 5-Fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone
  • CAL-101(IDELALISIB) AL-101
  • CAL-101(IDELALISIB)
  • AL-101
  • CAL-101, >=98%
  • IDELALISIB; CAL-101; GS-1101; GS 1101; GS1101;CAL101
  • CS-34
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  • 5-Fluoro-3-phenyl-2-[1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone
  • CAL-101 1KG
  • CAL-11
  • Idelalisib (This product is only available in Japan.)
  • CAL-101, 99%, a selective p110δ inhibitor
  • 4(3H)-Quinazolinone, 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-
  • -101
  • CAL-101 USP/EP/BP
  • Idelalisib (CAL101, Zydelig, GS1101)
  • 5-Fluoro-3-phenyl-2-[1-(9H-purin-6-ylamino)propyl]-4(3H)-qui...
  • Idelalisib,PI3K,CAL101,CAL 101,GS 1101,Phosphoinositide 3-kinase,Autophagy,Inhibitor,inhibit,GS1101
  • (S)-2-(1-((9H-Purin-6-yl)ami)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
  • Dabrafenib Mesilate
  • (S)-2-(1-((7H-purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
  • 870281-82-6
  • 10870281-82-6
  • C22H18FN7O
  • Akt
  • mTOR
  • PI3K
  • API
  • API
  • Inhibitors
  • Inhibitor