AC480 (BMS599626)
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 |
|---|---|---|
| 250mg | $1060 | Check With Us |
| 500mg | $1650 | Check With Us |
| 1g | $2475 | Check With Us |
: Cat #: V0554 CAS #: 714971-09-2 Purity ≥ 98%
Description: AC480 (also known as BMS-599626) is a novel, potent, orally bioavailable, selective and efficacious inhibitor of HER1/2 (human epidermal growth factor receptors) with potential anticancer activity.
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| Molecular Weight (MW) | 530.55 |
|---|---|
| Molecular Formula | C27H27FN8O3 |
| CAS No. | 714971-09-2 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 113 mg/mL (213.0 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 20 mg/mL (37.7 mM) | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL |
| SMILES Code | O=C(OC[C@H]1NCCOC1)NC2=CN3N=CN=C(NC4=CC5=C(N(CC6=CC=CC(F)=C6)N=C5)C=C4)C3=C2C |
| Synonyms | BMS-599626; BMS599626; BMS 599626; AC 480; AC-480; AC 480 hydrochloride; BMS599626 HCl; BMS599626 hydrochloride; AC480; AC 480 HCl; |
| Protocol | In Vitro | BMS-599626 abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 (IC50=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both). BMS-599626 inhibits the proliferation of tumor cells that are dependent on HER1/HER2 signaling. BMS-599626 (0.03-8 μM; 1 huors) results in the inhibition of receptor autophosphorylation, as well as MAPK phosphorylation, with IC50s of 0.3 and 0.22 μM, respectively, in Sal2 cells which express a CD8HER2 fusion protein. |
|---|---|---|
| In Vivo | BMS599626 treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, and KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast and N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 and L2987). BMS-599626 (60-240 mg/kg; p.o.; daily for 14 days) results in a dose-dependent inhibition of Sal2 tumor growth. |
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 | 1.8848 mL | 9.4242 mL | 18.8484 mL | 37.6967 mL |
| 5mM | 0.3770 mL | 1.8848 mL | 3.7697 mL | 7.5393 mL |
| 10mM | 0.1885 mL | 0.9424 mL | 1.8848 mL | 3.7697 mL |
| 20mM | 0.0942 mL | 0.4712 mL | 0.9424 mL | 1.8848 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
+
%ddH2O
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Method for preparing DMSO master liquid:
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,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.