4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl-
- Product Name
- 4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl-
- CAS No.
- 2160546-07-4
- Chemical Name
- 4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl-
- Synonyms
- BBP398;BBP-398;BBP 398;IACS13909;IACS15509;IACS-15509;IACS 15509;LACS-13909;BBP- 398 (IACS-13909);IACS-13909, 10 mM in DMSO
- CBNumber
- CB18093166
- Molecular Formula
- C17H18Cl2N6
- Formula Weight
- 377.27
- MOL File
- 2160546-07-4.mol
4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl- Property
- Boiling point:
- 577.3±50.0 °C(Predicted)
- Density
- 1.402±0.06 g/cm3(Predicted)
- solubility
- DMSO: Sparingly Soluble: 1-10 mg/ml
Ethanol: Sparingly Soluble: 1-10 mg/ml - form
- Solid
- pka
- 8.00±0.50(Predicted)
- color
- White to yellow
N-Bromosuccinimide Price
- Product number
- CS-0136474
- Product name
- IACS-13909
- Purity
- 99.93%
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CS-0136474
- Product name
- IACS-13909
- Purity
- 99.93%
- Packaging
- 10mg
- Price
- $500
- Updated
- 2021/12/16
- Product number
- CS-0136474
- Product name
- IACS-13909
- Purity
- 99.93%
- Packaging
- 25mg
- Price
- $1050
- Updated
- 2021/12/16
- Product number
- 020571
- Product name
- IACS-13909
- Packaging
- 003
- Price
- $2400
- Updated
- 2021/12/16
- Product number
- 020571
- Product name
- IACS-13909
- Packaging
- 001
- Price
- $700
- Updated
- 2021/12/16
4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl- Chemical Properties,Usage,Production
Uses
IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers[1].
in vivo
IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing[1].
| Animal Model: | NSG mice (20-28 g) injected with KYSE-520 cells[1] |
| Dosage: | 70 mg/kg |
| Administration: | Oral administration; daily; for 21 days |
| Result: | Potently suppressed tumor growth in mice. |
References
[1] Yuting Sun, et al. Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib. Cancer Res. 2020 Nov 1;80(21):4840-4853. DOI:10.1158/0008-5472.CAN-20-1634
[2] BARBARA CZAKO*. Discovery of 6-[(3S,4S)-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor[J]. Journal of Medicinal Chemistry, 2021, 64 20: 15141-15169. DOI: 10.1021/acs.jmedchem.1c01132
4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl- Preparation Products And Raw materials
Raw materials
Preparation Products
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