5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1-[1-[15-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-1-oxo-4,7,10,13-tetraoxapentadec-1-yl]-4-piperidinyl]-1,4,6,7-tetrahydro-N-methyl-
- CAS No.
- 2484739-25-3
- Chemical Name:
- 5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1-[1-[15-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-1-oxo-4,7,10,13-tetraoxapentadec-1-yl]-4-piperidinyl]-1,4,6,7-tetrahydro-N-methyl-
- Synonyms
- dCBP-1;Inhibitor,p300,multiple,CRBN,myeloma,cell,degrader,PROTACs,MYC,CBP,inhibit,dCBP 1,dCBP1,heterobifunctional,Epigenetic Reader Domain,dCBP-1;3-(7-(Difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-1-(1-(1-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-3,6,9,12-tetraoxapentadecan-15-oyl)piperidin-4-yl)-N-methyl-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide;5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1-[1-[15-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-1-oxo-4,7,10,13-tetraoxapentadec-1-yl]-4-piperidinyl]-1,4,6,7-tetrahydro-N-methyl-
- CBNumber:
- CB28383268
- Molecular Formula:
- C51H63F2N11O10
- Molecular Weight:
- 1028.11
- MDL Number:
- MFCD34471098
- MOL File:
- 2484739-25-3.mol
5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1-[1-[15-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-1-oxo-4,7,10,13-tetraoxapentadec-1-yl]-4-piperidinyl]-1,4,6,7-tetrahydro-N-methyl- Properties
Density | 1.47±0.1 g/cm3(Predicted) |
---|---|
storage temp. | Store at -20°C, sealed storage, away from moisture and light |
solubility | DMSO : 50 mg/mL (48.63 mM; ultrasonic and warming and heat to 80°C) |
form | Solid |
pka | 10.80±0.40(Predicted) |
color | Light yellow to yellow |
InChIKey | ILVRLRGBSSFKIE-UHFFFAOYSA-N |
SMILES | C1N(C(NC)=O)CCC2N(C3CCN(C(=O)CCOCCOCCOCCOCCNC4C=CC5=C(C=4)C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)N=C(N3C4=C(C=C(C5=CN(C)N=C5)C(C(F)F)=C4)CCC3)C1=2 |
5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1-[1-[15-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-1-oxo-4,7,10,13-tetraoxapentadec-1-yl]-4-piperidinyl]-1,4,6,7-tetrahydro-N-methyl- Chemical Properties,Uses,Production
Biological Activity
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression[1]. dCBP-1 (10-1000 nM; 6 hours) treatment shows near-complete degradation of p300/CBP in MM1S cells. dCBP-1 is also able to induce near-complete p300/CBP degradation across other multiple myeloma cell lines tested, including MM1R, KMS-12-BM, and KMS34[1].Treatment of the human haploid cell line HAP1 for 6 h with dCBP-1 reveals almost complete loss of both CBP and p300 between 10 and 1000 nM doses. A time course analysis with 250 nM dCBP-1 revealed almost complete degradation of p300/CBP within an hour of treatment[1].
References
[1]. Raghu Vannam, et al. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell Chem Biol. 2020 Dec 31;S2451-9456(20)30513-4.
5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1-[1-[15-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-1-oxo-4,7,10,13-tetraoxapentadec-1-yl]-4-piperidinyl]-1,4,6,7-tetrahydro-N-methyl- Preparation Products And Raw materials
Raw materials
Preparation Products
5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1-[1-[15-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-1-oxo-4,7,10,13-tetraoxapentadec-1-yl]-4-piperidinyl]-1,4,6,7-tetrahydro-N-methyl- Suppliers
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