A Bcl-2 and Bcl-2G101V inhibitor
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Sonrotoclax

Item No. 44268

Technical Information
Formal Name
N-[[4-[[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino]-3-nitrophenyl]sulfonyl]-4-[2-[(2S)-2-[2-(1-methylethyl)phenyl]-1-pyrrolidinyl]-7-azaspiro[3.5]non-7-yl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-benzamide
CAS Number
2383086-06-2
Synonyms
  • BGB-11417
Molecular Formula
C49H59N7O7S
Formula Weight
Purity
≥98%
Formulation
A solid
Acetonitrile: Slightly soluble: 0.1-1 mg/mlChloroform: Slightly soluble: 0.1-1 mg/ml
SMILES
CC(C1=C(C=CC=C1)[C@H]2N(CCC2)C3CC4(C3)CCN(CC4)C5=CC(OC6=CN=C7NC=CC7=C6)=C(C(NS(=O)(C8=CC([N+]([O-])=O)=C(C=C8)NC[C@H]9CC[C@@](C)(CC9)O)=O)=O)C=C5)C
InChi Code
InChI=1S/C49H59N7O7S/c1-32(2)39-7-4-5-8-40(39)43-9-6-22-55(43)36-28-49(29-36)19-23-54(24-20-49)35-10-12-41(45(26-35)63-37-25-34-16-21-50-46(34)52-31-37)47(57)53-64(61,62)38-11-13-42(44(27-38)56(59)60)51-30-33-14-17-48(3,58)18-15-33/h4-5,7-8,10-13,16,21,25-27,31-33,36,43,51,58H,6,9,14-15,17-20,22-24,28-30H2,1-3H3,(H,50,52)(H,53,57)/t33-,43-,48-/m0/s1
InChi Key
ZQTKOYMWCCSKON-XKXNWSITSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Sonrotoclax is an inhibitor of wild-type Bcl-2 and Bcl-2 containing a glycine-to-valine mutation at residue 101 (Bcl-2G101V; IC50s = 0.019 and 0.34 nM, respectively).1 It is selective for Bcl-2 over Bcl-xL (IC50 = 28 nM). Sonrotoclax reduces the viability of Bcl-2-dependent RS4;11 acute lymphoblastic leukemia (ALL) cells but not Bcl-2-independent MOLT-4 ALL cells (IC50s = 0.56 and 2,493 nM, respectively). It also reduces the viability of RS4;11 cells expressing the Bcl-2G101V mutation (IC50 = 7.7 nM).2 Sonrotoclax (7.5 and 25 mg/kg per day) induces intratumoral apoptosis and reduces tumor volume in an RS4;11 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Guo, Y., Xue, H., Hu, N., et alDiscovery of the clinical candidate sonrotoclax (BGB-11417), a highly potent and selective inhibitor for both WT and G101V mutant Bcl-2. J. Med. Chem. 67(10), 7836-7858 (2024).

    2. Liu, J., Li, S., Wang, Q., et alSonrotoclax overcomes BCL2 G101V mutation-induced venetoclax resistance in preclinical models of hematologic malignancy. Blood 143(18), 1825-1836 (2024).