A-1331852
- Product Name
- A-1331852
- CAS No.
- 1430844-80-6
- Chemical Name
- A-1331852
- Synonyms
- CS-2498;A-1331852;A 1331852;A1331852;A-1331852,Inhibitor,inhibit,A1331852,Bcl-2 Family,A 1331852;6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-(adamantylmethyl)-5-methyl-1H-pyrazol-4-yl)picolinic acid;3-(1-(Adamantan-1-ylmethyl)-5-methyl-1H-pyrazol-4-yl)-6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)picolinic acid;6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl]-3-[5-methyl-1-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-1H-pyrazol-4-yl]pyridine-2-carboxylic acid;2-Pyridinecarboxylic acid, 6-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-3-[5-methyl-1-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-1H-pyrazol-4-yl]-
- CBNumber
- CB83070794
- Molecular Formula
- C38H38N6O3S
- Formula Weight
- 658.81
- MOL File
- 1430844-80-6.mol
A-1331852 Property
- Melting point:
- >161oC (dec.)
- Density
- 1.50±0.1 g/cm3(Predicted)
- storage temp.
- -20°C Freezer
- solubility
- Acetonitrile (Slightly, Heated), DMSO (Slightly)
- pka
- 8.88±0.70(Predicted)
- form
- Solid
- color
- Pale Yellow to Light Beige
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing 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.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 22963
- Product name
- A-1331852
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $97
- Updated
- 2024/03/01
- Product number
- 22963
- Product name
- A-1331852
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $193
- Updated
- 2024/03/01
- Product number
- 22963
- Product name
- A-1331852
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $337
- Updated
- 2024/03/01
- Product number
- A100900
- Product name
- A-1331852
- Packaging
- 25mg
- Price
- $275
- Updated
- 2021/12/16
- Product number
- B6164
- Product name
- A-1331852
- Packaging
- 10mg
- Price
- $315
- Updated
- 2021/12/16
A-1331852 Chemical Properties,Usage,Production
Description
A-1331852 is an orally bioavailable Bcl-xL inhibitor that selectively binds Bcl-xL over Bcl-2, Mcl-1, and Bcl-W (Kis = <0.01, 6, 142, and 4 nM, respectively). It inhibits growth of Bcl-xL-dependent MOLT-4, but not Bcl-2-dependent RS4;11, acute lymphocytic leukemia cells in vitro (EC50s = 6 and >5,000 nM, respectively). A-1331852 (25 mg/kg twice per day) inhibits tumor growth in a MOLT-4 mouse xenograft model. It also inhibits tumor growth and increases the antitumor activity of docetaxel in MDA-MB-231 LC3 metastatic breast cancer and NCI-H1650 non-small cell lung cancer mouse xenograft models when administered at a dose of 25 mg/kg. A-1331852 also increases venetoclax inhibition of tumor growth in an NCI-H1963.FP5 small cell lung cancer mouse xenograft model.
Uses
A-1331852 is a substituted benzothiazole that can serve as an anti-apoptotic Bcl-xL protein inhibitor and apoptosis-inducing agent useful in the treatment of cancer, immune and autoimmune diseases.
in vitro
a-1331852 was identified as a potent bcl-xl inhibitor demonstrating cellular activity 10- to 50-fold more potent than its analog a-1155463 and the previouly reported bcl-xl inhibitor, navitoclax, respectively. moreover, a-1331852 could selectively disrupt bcl-xl–bim complexes and induce the apoptosis hallmarks in bcl-xl–dependent molt-4 cells with median ic50 values in the low nanomolar range but did not affect mef cells without bak or bax [1].
in vivo
previous animal study found that a-1331852 could demonstrate antitumor efficacy in the molt-4 xenograft model, such as tumor regressions as a single agent. in addition, in the nci-h1963.fp5 xenograft model of sclc, it was found that a-1331852 combined with venetoclax was able to recapitulate the efficacy of navitoclax [1].
storage
Store at -20°C
References
[1] leverson jd et al. exploiting selective bcl-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. sci transl med. 2015 mar 18;7(279):279ra40. doi: 10.1126/scitranslmed.aaa4642.
A-1331852 Preparation Products And Raw materials
Raw materials
Preparation Products
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