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| Description |
| ARQ 531 is an investigational, orally bioavailable, potent and reversible inhibitor of both wild type and C481S-mutant Bruton’s tyrosine kinase (BTK).B-cell malignancies, like chronic lymphocytic lymphoma (CLL), Waldenstrom’s macroglobulinemia, diffuse large B-cell lymphoma (DLBCL) and mantle cell lymphoma (MCL) are driven by BTK. The only approved BTK inhibitor, ibrutinib, is irreversible and makes a covalent bond with the C481 residue of the targeted protein. Although ibrutinib has demonstrated excellent responses in patients with elevated BCR signaling, clinical resistance has been observed, and the BTK-C481S mutation is emerging as a predominant mechanism of resistance. As a reversible inhibitor, ARQ 531 does not require interaction with the C481 residue, a binding site essential for irreversible ibrutinib binding to BTK, thus positioning ARQ 531 as a targeted therapy for CLL, DLBCL, MCL patients harboring C481S-mutant BTK who have developed resistance to irreversible BTK inhibitors. |
| Chemical Structure |
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| Chemical Name |
| (2-Chloro-4-phenoxyphenyl)(4-(((3R,6S)-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)amino)-7H-pyrrolo(2,3-d)pyrimidin-5-yl)methanone |
| Theoretical Analysis |
XingMo Cat#:XM727
Product Name:ARQ-531
Synonyms:ARQ531
CAS#:2095393-15-8
Chemical Formula:C25H23ClN4O4
Exact Mass:478.14
Molecular Weight:478.93
Purity:>98%
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| Technical Data |
Appearance: solid powder
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 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years)
Solubility: Soluble in DMSO, not in water
Shelf Life:
>2 years if stored properly.
Drug Formulation:
This drug may be formulated in DMSO
Stock Solution Storage:
0 - 4 ℃ for short term (days to weeks), or -20 ℃ for long term (months). |
WARNING: This product is for research use only, not for human or veterinary use
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