Brigatinib (AP26113)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $510 | Check With Us |
| 1g | $805 | Check With Us |
| 5g | $2040 | Check With Us |
: Cat #: V0607 CAS #: 1197953-54-0 Purity ≥ 99%
Description: Brigatinib (formerly AP26113; AP-26113; ALK-IN-1; trade name: Alunbrig) is an orally bioavailable, FDA-approved and selective ALK (anaplastic lymphoma kinase) inhibitor with potential antineoplastic activity.
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| Molecular Weight (MW) | 584.09 |
|---|---|
| Molecular Formula | C₂₉H₃₉ClN₇O₂P |
| CAS No. | 1197953-54-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 45 mg/mL (85.1 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 106 mg/mL (200.4 mM) | |
| Solubility In Vivo | NMP+polyethylene glycol 300 (10+90, v+v): 1 mg/mL |
| SMILES Code | CN1CCN(C2CCN(C3=CC=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5P(C)(C)=O)=N4)C(OC)=C3)CC2)CC1 |
| Synonyms | AP-26113; AP 26113; Brigatinib-analog; AP26113; Brigatinib; Alunbrig |
| Protocol | In Vitro | Brigatinib potently inhibits the in vitro kinase activity of ALK (IC50, 0.6 nM) and all five mutant variants tested, including G1202R (IC50, 0.6-6.6 nM). Brigatinib demonstrates a high degree of selectivity, only inhibiting 11 additional native or mutant kinases with IC50 <10 nM. These include ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR (L858R; IC50, 1.5-2.1 nM). Brigatinib exhibits more modest activity against EGFR with a T790M resistance mutation (L858R/T790M), native EGFR, IGF1R, and INSR (IC50, 29-160 nM) and does not inhibit MET (IC50 >1000 nM). In cellular assays, brigatinib inhibits ALK and ROS1 with IC50s of 14 and 18 nM, respectively. Brigatinib inhibits FLT3 and IGF-1R with about 11-fold lower potency (IC50, 148-158 nM) and inhibits mutant variants of FLT3 and EGFR with 15- to 35-fold lower potency (IC50, 211-489 nM). Brigatinib inhibits cell growth with GI50 values ranging from 503 to 2,387 nM in three ALK-negative ALCL and NSCLC cell lines. |
|---|---|---|
| In Vivo | Brigatinib (10, 25, or 50 mg/kg once daily, p.o.) leads to a dose-dependent inhibition of tumor growth in ALK+ Karpas-299 (ALCL) and H2228 (NSCLC) xenograft mouse models. Brigatinib markedly enhances survival of mice bearing ALK+ brain tumors compared with PF-02341066. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.7121 mL | 8.5603 mL | 17.1206 mL | 34.2413 mL |
| 5mM | 0.3424 mL | 1.7121 mL | 3.4241 mL | 6.8483 mL |
| 10mM | 0.1712 mL | 0.8560 mL | 1.7121 mL | 3.4241 mL |
| 20mM | 0.0856 mL | 0.4280 mL | 0.8560 mL | 1.7121 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.