ND-646
- Product Name
- ND-646
- CAS No.
- 1434639-57-2
- Chemical Name
- ND-646
- Synonyms
- ND-646;CPD5077;ND646;ND 646;ND646 ,S8377;ND-646, 10 mM in DMSO;Acetyl-CoA Carboxylase,ND 646,ND646,ND-646,ACC, Acetyl Coenzyme A Carboxylase,Inhibitor,inhibit;2-[1-[(2R)-2-(2-methoxyphenyl)-2-(oxan-4-yloxy)ethyl]-5-methyl-6-(1,3-oxazol-2-yl)-2,4-dioxo-1H,2H,3H,4H-thieno[2,3-d]pyrimidin-3-yl]-2-methylpropanamide;2-[1-[(2~{r})-2-(2-Methoxyphenyl)-2-(Oxan-4-Yloxy)ethyl]-5-Methyl-6-(1,3-Oxazol-2-Yl)-2,4-Bis(Oxidanylidene)thieno[2,3-D]pyrimidin-3-Yl]-2-Methyl-Propanamide;1,4-Dihydro-1-[(2R)-2-(2-methoxyphenyl)-2-[(tetrahydro-2H-pyran-4-yl)oxy]ethyl]-α,α,5-trimethyl-6-(2-oxazolyl)-2,4-dioxothieno[2,3-d]pyrimidine-3(2H)-acetamide;Thieno[2,3-d]pyrimidine-3(2H)-acetamide, 1,4-dihydro-1-[(2R)-2-(2-methoxyphenyl)-2-[(tetrahydro-2H-pyran-4-yl)oxy]ethyl]-α,α,5-trimethyl-6-(2-oxazolyl)-2,4-dioxo-
- CBNumber
- CB23358870
- Molecular Formula
- C28H32N4O7S
- Formula Weight
- 568.64
- MOL File
- 1434639-57-2.mol
ND-646 Property
- Boiling point:
- 801.8±75.0 °C(Predicted)
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml; Ethanol: 20 mg/ml
- form
- A solid
- pka
- 15.52±0.50(Predicted)
- color
- White to off-white
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.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-7887
- Product name
- ND-646
- Purity
- 99.53%
- Packaging
- 1mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-7887
- Product name
- ND-646
- Purity
- 99.53%
- Packaging
- 5mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-7887
- Product name
- ND-646
- Purity
- 99.53%
- Packaging
- 10mg
- Price
- $750
- Updated
- 2021/12/16
- Product number
- CS-7887
- Product name
- ND-646
- Purity
- 99.53%
- Packaging
- 25mg
- Price
- $1350
- Updated
- 2021/12/16
- Product number
- CS-7887
- Product name
- ND-646
- Purity
- 99.53%
- Packaging
- 50mg
- Price
- $1950
- Updated
- 2021/12/16
ND-646 Chemical Properties,Usage,Production
Uses
ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively.
in vivo
To explore the impact of chronic ND-646 treatment on NSCLC tumor growth and to determine the efficacy of twice-daily dosing, athymic nude mice bearing established A549 subcutaneous tumors are treated orally with either vehicle twice daily (BID), 25 mg/kg ND-646 once daily (QD), 25 mg/kg ND-646 BID or 50 mg/kg ND-646 QD for 31 days. ND-646 at 25 mg/kg QD is ineffective at inhibiting tumor growth. However, ND-646 administered at 25 mg/kg BID or 50 mg/kg QD significantly inhibits subcutaneous A549 tumor growth. ND-646 is well tolerated throughout the treatment period, with no significant weight loss occurring after chronic ND-646 dosing, suggesting that the maximum tolerated dose (MTD) has not been reached. Mice are sacrificed at 1 hr post final dose and tissues are either prepared for immunohistochemistry (IHC) or immunoblot analysis. Tumors treated with all doses of ND-646 have lost detection of P-ACC at 1 hr, demonstrating effective tumor penetration and acute ACC inhibition by ND-646. Notably, only at the doses of ND-646 that lead to significant tumor growth inhibition (25 mg/kg BID and 50 mg/kg QD) is significant elevation of P-EIF2αS51 expression observed in tumor lysates[1].
References
[1] Svensson RU, et al. Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small-cell lung cancer in preclinical models. Nat Med. 2016 Oct;22(10):1108-1119. DOI:10.1038/nm.4181
ND-646 Preparation Products And Raw materials
Raw materials
Preparation Products
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