1. PROTAC Protein Tyrosine Kinase/RTK
  2. SNIPERs Bcr-Abl
  3. SNIPER(ABL)-039

SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively.

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SNIPER(ABL)-039

SNIPER(ABL)-039 Chemische Struktur

CAS. Nr. : 2222354-29-0

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Beschreibung

SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively[1].

IC50 & Target[1]

Abl

0.54 nM (IC50)

cIAP1

10 nM (IC50)

cIAP2

12 nM (IC50)

XIAP

50 nM (IC50)

SNIPER

 

Abl

10 nM (DC50)

Cellular Effect
Cell Line Type Value Description References
K562 DC50
>=3 nM
Compound: 4; SNIPER(ABL)-39
Protac activity at BCR-ABL/XIAP in human K562 cells assessed as induction of ABL protein degradation after 6 hrs by Western blot analysis
Protac activity at BCR-ABL/XIAP in human K562 cells assessed as induction of ABL protein degradation after 6 hrs by Western blot analysis
[PMID: 31047748]
Molekulargewicht

1114.77

Formel

C54H68ClN11O9S2

CAS. Nr.
SMILES

CC1=C(NC(C2=CN=C(NC3=CC(N4CCN(C(COCCOCCOCCOC5=CC(C(C6=CSC([C@H]7N(C([C@H](C8CCCCC8)NC([C@H](C)NC)=O)=O)CCC7)=N6)=O)=CC=C5)=O)CC4)=NC(C)=N3)S2)=O)C(Cl)=CC=C1

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

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