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ALK-IN-1

Cat. No. M5309
ALK-IN-1 Structure
Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 155 In stock
50mg USD 390 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Brigatinib and AP26113-analog have similar potency against the triple-mutant EGFR with IC50 values of <100 nM. AP26113-analog suppresses phosphorylation of EGFR and its downstream signalling pathway in cells expressing all types of EGFR mutations.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 529.01
Formula C26H34ClN6O2P
CAS Number 1197958-12-5
Purity >98%
Solubility 45 mg/mL in DMSO
Storage at -20°C
References

Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer.
Uchibori K, et al. Nat Commun. 2017 Mar 13;8:14768. PMID: 28287083.

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase
Wei-Sheng Huang, et al. Journal of Medicinal Chemistry. 2016 May 26;59(10):4948-64. PMID: 27144831.

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LDK378 dihydrochloride

LDK378 2Hcl (Ceritinib) is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.

Entrectinib (RXDX-101)

Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.

Crizotinib hydrochloride

Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM). Crizotinib is useful in treatment of anaplastic large-cell lymphoma.

Brigatinib

Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ALK-IN-1 supplier, ALK, inhibitors

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