WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H123937
CAS#: N/A
Description: JET-209 is an exceptionally potent PROTAC degrader of CBP/p300. JET-209, achieved a half-maximal degradation (DC50) value of 0.05 nM for CBP and 0.2 nM for p300 with maximum degradation (Dmax) >95% for both proteins in the RS4;11 leukemia cell line after 4 h of treatment. JET-209 achieved subnanomolar to low nanomolar DC50 values in the inhibition of cell growth in several representative acute leukemia cell lines and was much more potent than CBP/p300 bromodomain and catalytic domain inhibitors. JET-209 effectively inhibited tumor growth in xenograft tumor models at tolerated dose schedules.
Hodoodo Cat#: H123937
Name: JET-209
CAS#: N/A
Chemical Formula: C46H47N9O6
Exact Mass: 821.36
Molecular Weight: 821.940
Elemental Analysis: C, 67.22; H, 5.76; N, 15.34; O, 11.68
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Synonym: JET-209; JET 209; JET209
IUPAC/Chemical Name: 5-(8-(5-acetyl-1-(tetrahydro-2H-pyran-4-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)isoquinolin-3-yl)-N-(1-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperidin-4-yl)picolinamide
InChi Key: OGNHAQXAAGMVOV-UHFFFAOYSA-N
InChi Code: InChI=1S/C46H47N9O6/c1-27(56)53-18-13-40-37(26-53)43(51-55(40)32-14-19-61-20-15-32)35-4-2-3-28-22-39(48-24-36(28)35)29-5-8-38(47-23-29)44(58)49-31-11-16-52(17-12-31)33-6-7-34-30(21-33)25-54(46(34)60)41-9-10-42(57)50-45(41)59/h2-8,21-24,31-32,41H,9-20,25-26H2,1H3,(H,49,58)(H,50,57,59)
SMILES Code: O=C(NC1CCN(C2=CC3=C(C(N(C(CC4)C(NC4=O)=O)C3)=O)C=C2)CC1)C5=NC=C(C6=CC7=C(C=N6)C(C8=NN(C9CCOCC9)C%10=C8CN(C(C)=O)CC%10)=CC=C7)C=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
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 821.94 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
Thomas JE 2nd, Wang M, Jiang W, Wang M, Wang L, Wen B, Sun D, Wang S. Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins. J Med Chem. 2023 Jun 5. doi: 10.1021/acs.jmedchem.3c00492. Epub ahead of print. PMID: 37276143.
