A Bcl-2 inhibitor
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Lisaftoclax

Item No. 44963

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[[6-(4-chlorophenyl)spiro[3.5]non-6-en-7-yl] methyl]-1-piperazinyl]-N-[[4-[[(2S)-1,4-dioxan-2-ylmethyl]amino]-3- nitrophenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-benzamide
CAS Number
2180923-05-9
Synonyms
  • APG-2575
Molecular Formula
C45H48ClN7O8S
Formula Weight
882.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
ClC(C=C1)=CC=C1C(CC2(CCC2)CC3)=C3CN4CCN(C5=CC(OC6=CN=C7NC=CC7=C6)=C(C(NS(C8=CC([N+]([O-])=O)=C(NC[C@@H]9OCCOC9)C=C8)(=O)=O)=O)C=C5)CC4
InChi Code
InChI=1S/C45H48ClN7O8S/c46-33-4-2-30(3-5-33)39-25-45(12-1-13-45)14-10-32(39)28-51-16-18-52(19-17-51)34-6-8-38(42(23-34)61-35-22-31-11-15-47-43(31)49-26-35)44(54)50-62(57,58)37-7-9-40(41(24-37)53(55)56)48-27-36-29-59-20-21-60-36/h2-9,11,15,22-24,26,36,48H,1,10,12-14,16-21,25,27-29H2,(H,47,49)(H,50,54)/t36-/m0/s1
InChi Key
FNBXDBIYRAPDPI-BHVANESWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $349

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    5 mg

    $698

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    10 mg

    $873

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    Product Description

    Lisaftoclax is an inhibitor of Bcl-2 (Ki = <0.1 nM).1 It is selectively cytotoxic to diffuse large B cell lymphoma (DLBCL) cells with high Bcl-2 expression (IC50s = 0.014-0.384 µM) over those with low Bcl-2 and high Mcl-1 expression (IC50s = 1.11-10.343 µM). It induces apoptosis in OCI-LY8 and OCI-Ly19 cells at 5, 10, and 50 nM and induces M2-to-M1 repolarization in tumor-associated macrophages (TAMs).1,2 It reduces tumor growth in an OCI-LY8 DLBCL mouse xenograft model when administered at doses of 50 and 100 mg/kg.1 Lisaftoclax also enhances anti-programmed cell death protein 1 (PD-1) monoclonal antibody-induced reductions in tumor growth in an H1299 humanized mouse model of non-small cell lung cancer (NSCLC).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Luo, Q., Pan, W., Zhou, S., et al. A novel BCL-2 inhibitor APG-2575 exerts synthetic lethality with BTK or MDM2-p53 inhibitor in diffuse large B-cell lymphoma. Oncol. Res. 28(4), 331-344 (2020).

    2. Luo, F., Li, H., Ma, W., et al. The BCL-2 inhibitor APG-2575 resets tumor-associated macrophages toward the M1 phenotype, promoting a favorable response to anti-PD-1 therapy via NLRP3 activation. Cell. Mol. Immunol. 21(1), 60-79 (2024).