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Lisaftoclax

Cat. No. M22479
Lisaftoclax Structure
Synonym:

APG-2575; Bcl-2/Bcl-xl inhibitor 1

Size Price Availability Quantity
5mg USD 800  USD800 In stock
10mg USD 1220  USD1220 In stock
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Quality Control & Documentation
Biological Activity

Lisaftoclax (APG-2575) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.

Chemical Information
Molecular Weight 882.42
Formula C45H48ClN7O8S
CAS Number 2180923-05-9
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Sikander Ailawadhi, et al. Clin Cancer Res. Novel BCL-2 Inhibitor Lisaftoclax in Relapsed or Refractory Chronic Lymphocytic Leukemia and Other Hematologic Malignancies: First-in-Human Open-Label Trial

[2] Yifan Zhai, et al. Clin Cancer Res. Lisaftoclax in Combination with Alrizomadlin Overcomes Venetoclax Resistance in Acute Myeloid Leukemia and Acute Lymphoblastic Leukemia: Preclinical Studies

[3] Jing Deng, et al. Clin Cancer Res. Lisaftoclax (APG-2575) Is a Novel BCL-2 Inhibitor with Robust Antitumor Activity in Preclinical Models of Hematologic Malignancy

[4] Douglas D Fang, et al. Transl Oncol. FLT3 inhibition by olverembatinib (HQP1351) downregulates MCL-1 and synergizes with BCL-2 inhibitor lisaftoclax (APG-2575) in preclinical models of FLT3-ITD mutant acute myeloid leukemia

Related Bcl-2 Products
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BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL.

Bim BH3, Peptide IV

Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins.

Bax inhibitor peptide, negative control

Bax inhibitor peptide, negative control is a inhibitor of Bax.

Bad BH3 (mouse)

Bad BH3 (mouse) is a biological active peptide.

Bid BH3 (80-99)

Bid BH3 (80-99) is a biological active peptide.

  Catalog
Abmole Inhibitor Catalog




Keywords: Lisaftoclax, APG-2575; Bcl-2/Bcl-xl inhibitor 1 supplier, Bcl-2, inhibitors, activators


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