SJ1008030
SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 can be used for the research of leukemia.
(Pink: JAK2 ligand (HY-15315); Blue: Cereblon ligand (HY-W834174); Black: linker).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 2863634-96-0
- Formule: C42H43N13O7S
- Masse moléculaire:873.94
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
IC50: 32.09 nM (MHH-CALL-4), 33.41 nM (MHH-CALL4-GSPT1-WT), 33.55 nM (MHH-CALL-4-GSPT1-G575N) [1]
SJ1008030 (compound 8) (72 h) shows activity in CRLF2r cell lines (MHH–CALL-4), with an IC50 of 5.4 nM[1]. SJ1008030 (0-4.3 μM; 72 h) degrades JAKs, GSPT1, and IKZF1 in a dose-dependent manner in MHH–CALL-4 cells[1]. SJ1008030 (0-10 μM; 24h) dose-dependently degrades JAK2 and GSPT1 protein in xenograft bone marrow SJBALL021415 cells, indicating the inhibition of JAK-STAT signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:The CRLF2r cell lines MHH–CALL-4, KOPN49, MHH–CALL-2, KOP N75, NALM-6 and 697
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Concentration:0-3 μM
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Incubation Time:72 hours
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Result:Showed best activity in MHH–CALL-4 cells with an EC50 value of 5.4 nM.
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Cell Line:MHH–CALL-4 cells
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Concentration:1 nM, 10 nM, 100 nM, 1 μM and 4.3 μM
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Incubation Time:72 hours
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Result:Significantly degradated JAK2 in MHH–CALL-4 cells dose-dependently while showed weakly effect to JAK1, JAK3 and GSPT1.
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Cell Line:Xenograft SJBALL021415 bone marrow cells
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Concentration:1, 10, 100, 1000 and 1000 nM
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Incubation Time:24 hours
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Result:Near-completely degradated JAK2 in a dose-dependent way while showed no effect on GSPT1.
Chemical Information
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CAS No. 2863634-96-0
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Masse moléculaire 873.94
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Formule C42H43N13O7S
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SMILES
O=S(CC)(N1CC(N2C=C(C=N2)C3=C4C=CNC4=NC(NC5=CC=C(C=C5)C(NCCN6CCN(CC6)C7=CC=C8C(N(C9CCC(NC9=O)=O)C(C8=C7)=O)=O)=O)=N3)(CC#N)C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)