Synonym
BR-101801; BR101801; BR 101801;
IUPAC/Chemical Name
(S)-4-((1-(4,8-dichloro-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-5(1H)-one
InChi Key
HIXUFHUKIOTXLJ-ZDUSSCGKSA-N
InChi Code
1S/C24H17Cl2N5O2/c1-13(30-23-19-17(32)10-11-27-22(19)28-12-29-23)21-20(26)15-8-5-9-16(25)18(15)24(33)31(21)14-6-3-2-4-7-14/h2-13H,1H3,(H2,27,28,29,30,32)/t13-/m0/s1
SMILES Code
C[C@H](NC1=C2C(=O)C=CN=C2NC=N1)C3=C(Cl)C4=CC=CC(Cl)=C4C(=O)N3C5=CC=CC=C5
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
478.33
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Park M, Ha J, Lee Y, Kwon Y, Choi SH, Kim BS, Jeong YK. BR101801 enhances the radiosensitivity of p53-deficient colorectal cancer cells by inducing G2/M arrest, apoptosis, and senescence in a p53-independent manner. Am J Cancer Res. 2023 Dec 15;13(12):5887-5900. PMID: 38187039; PMCID: PMC10767343.
2: Jeon B, Lee YJ, Shin J, Choi MJ, Lee CE, Son MK, Park JH, Kim BS, Kim HR, Jung KH, Cha JH, Hong SS. A combination of BR101801 and venetoclax enhances antitumor effect in DLBCL cells via c-Myc/Bcl-2/Mcl-1 triple targeting. Am J Cancer Res. 2023 Feb 15;13(2):452-463. PMID: 36895970; PMCID: PMC9989607.
3: Yoon YN, Lee E, Kwon YJ, Gim JA, Kim TJ, Kim JS. PI3Kδ/γ inhibitor BR101801 extrinsically potentiates effector CD8+ T cell-dependent antitumor immunity and abscopal effect after local irradiation. J Immunother Cancer. 2022 Mar;10(3):e003762. doi: 10.1136/jitc-2021-003762. PMID: 35288465; PMCID: PMC8921929.
4: Lee JH, Jeon B, Park M, Ha J, Kim SJ, Son MK, Wang S, Lee JH, Jeong YK. Synergistic radiosensitizing effect of BR101801, a specific DNA-dependent protein kinase inhibitor, in various human solid cancer cells and xenografts. Am J Cancer Res. 2021 Nov 15;11(11):5440-5451. PMID: 34873471; PMCID: PMC8640799.
