| Identification | Back Directory | [Name]
SD-36 | [CAS]
2429877-44-9 | [Synonyms]
SD-36
P-[[2-[[[(5S,8S,10aR)-8-[[[(1S)-4-amino-1-[[(diphenylmethyl)amino]carbonyl]-4-oxobutyl]amino]carbonyl]-3-[8-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]-1-oxo-7-octyn-1-yl]decahydro-6-oxopyrrolo[1,2-a][1,5]diazocin-5-yl]amino]carbonyl]-1H-indol-5-yl]difluoromethyl]phosphonic acid
Phosphonic acid, P-[[2-[[[(5S,8S,10aR)-8-[[[(1S)-4-amino-1-[[(diphenylmethyl)amino]carbonyl]-4-oxobutyl]amino]carbonyl]-3-[8-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]-1-oxo-7-octyn-1-yl]decahydro-6-oxopyrrolo[1,2-a][1,5]diazocin-5-yl]amino]carbonyl]-1H-indol-5-yl]difluoromethy... | [Molecular Formula]
C59H62F2N9O12P | [MDL Number]
MFCD32263414 | [MOL File]
2429877-44-9.mol | [Molecular Weight]
1158.17 |
| Chemical Properties | Back Directory | [density ]
1.50±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
1.75±0.10(Predicted) | [color ]
White to off-white | [InChIKey]
JKCSCHXVWPSGBG-FBTHHHGANA-N |
| Hazard Information | Back Directory | [Uses]
SD-36 is a potent, selective and efficacious PROTAC (proteolysis targeting chimera) degrader of STAT3 (Signal transducer and activator of transcription 3) protein. | [in vivo]
SD-36 (25-100 mg/kg; i.v.; weekly dosing for 4 weeks) achieves complete and long-lasting tumor regression in mice[1].
SD-36 effectively inhibits tumor growth at 25 and 50 mg/kg administered on day 1, 3, and 5 per week and achieved complete tumor regression at 100 mg/kg with the same schedule in the SU-DHL-1 xenograft model[1].
SD-36 at 50 mg/kg 3 times per week completely inhibits tumor growth in the SUP-M2 tumor model[1]. | Animal Model: | SCID female mice (MOLM-16 xenograft model)[1] | | Dosage: | 25, 50, 100 mg/kg | | Administration: | i.v.; weekly dosing for 4 weeks | | Result: | At 25 and 50 mg/kg weekly dosing for 4 weeks effectively inhibited tumor growth. At either 100 mg/kg weekly or 50 mg/kg twice weekly for 4 weeks induced complete tumor regression. |
| [IC 50]
STAT3: 50 nM (Kd); Cereblon |
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