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Asciminib

Cat. No. M9259
Asciminib Structure
Synonym:

ABL001

Size Price Availability Quantity
5mg USD 124  USD155 In stock
10mg USD 196  USD245 In stock
50mg USD 440  USD550 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Asciminib (ABL001) selectively inhibited the growth of CML and Ph+ ALL cells with potencies ranging from 1-10nM range. Asciminib was tested for activity against clinically observed mutations and found to be active in the low nM range. In the KCL-22 mouse xenograft model, Asciminib displayed potent anti-tumor activity with complete tumor regression observed and a clear dose-dependent correlation with pSTAT5 inhibition. The oral bioavailability of ABL001 in mouse and rat are 35% and 27% respectively when dosed at 30 mg/kg p.o. While in dogs the oral BA of ABL001 is 111% (15 mg/kg, p.o).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 449.84
Formula C20H18ClF2N5O3
CAS Number 1492952-76-7
Purity >99%
Solubility DMSO ≥ 40 mg/mL
Storage at -20°C
References

[1] Wylie AA, et al. Nature. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.

[2] Andrew Wylie, et al. Blood. ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Resistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia

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Keywords: Asciminib, ABL001 supplier, Src-bcr-Abl, inhibitors

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