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SIAIS178 is a selective PROTAC degrader targeting BCR-ABL with an IC50 of 24 nM. It degrades BCR-ABL protein by recruiting the VHL E3 ubiquitin ligase, inhibiting leukaemia cell growth in vitro and causing regression of K562 xenograft tumours.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $163 | In Stock | |
5 mg | $396 | In Stock | |
10 mg | $538 | In Stock | |
25 mg | $987 | In Stock | |
50 mg | $1,590 | In Stock | |
100 mg | $2,280 | In Stock | |
200 mg | $2,970 | In Stock | |
1 mL x 10 mM (in DMSO) | $436 | In Stock |
Description | SIAIS178 is a selective PROTAC degrader targeting BCR-ABL with an IC50 of 24 nM. It degrades BCR-ABL protein by recruiting the VHL E3 ubiquitin ligase, inhibiting leukaemia cell growth in vitro and causing regression of K562 xenograft tumours. |
Targets&IC50 | VHL:24 nM, BCR-ABL:24 nM |
In vitro | Methods: K562 cells were treated with SIAIS178 (1, 3, 10, 30, 100 nM, 16 hours) and BCR-ABL protein expression was detected by Western blot. Results: SIAIS178 significantly reduced BCR-ABL protein levels in a concentration-dependent manner. [1] |
In vivo | Methods: SIAIS178 (5, 15, and 45 mg/kg) was used to treat K562-Luc NOD/SCID mice and investigate its effect on tumor progression in vivo. Results: SIAIS178 attenuated tumor progression in a dose-dependent manner as determined by serial volume measurements. [1] |
Synonyms | SIAI S178 |
Molecular Weight | 1012.68 |
Formula | C50H62ClN11O6S2 |
Cas No. | 2376047-73-1 |
Smiles | C([C@@H](NC(CCCCCCC(=O)N1CCN(CC1)C=2C=C(NC=3SC(C(NC4=C(C)C=CC=C4Cl)=O)=CN3)N=C(C)N2)=O)[C@](C)(C)C)(=O)N5[C@H](C(NCC6=CC=C(C=C6)C7=C(C)N=CS7)=O)C[C@@H](O)C5 |
Relative Density. | 1.335 g/cm3 (Predicted) |
Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 245 mg/mL (241.93 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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