A-966492
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1150 | Check With Us |
| 500mg | $1750 | Check With Us |
| 1g | $2625 | Check With Us |
: Cat #: V0313 CAS #: 934162-61-5 Purity ≥ 98%
Description: A-966492 is a selective and orally bioavailable PARP [poly(ADP-ribose) polymerase] inhibitor with potential anticancer activity.
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| Molecular Weight (MW) | 324.35 |
|---|---|
| Molecular Formula | C18H17FN4O |
| CAS No. | 934162-61-5 |
| Storage | -20℃ for 3 years in powder formrr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 64 mg/mL (197.3 mM)rr |
| Water:<1 mg/mLrr | |
| Ethanol: <1 mg/mL | |
| Synonyms | A-966492; A966492; A 966492. |
| Protocol | In Vitro | A-966492 is one of the most potent PARP inhibitors. A-966492 displays excellent potency against the PARP-1 enzyme with a Ki of 1 nM and an EC50 of 1 nM in a whole cell assay. A-966492 significantly enhances the efficacy of TMZ in a dose-dependent manner. In addition, A-966492 is orally bioavailable across multiple species, crosses the blood−brain barrier, and appears to distribute into tumor tissue. A-966492 represents a promising, structurally diverse benzimidazole analogue and is being further characterized preclinically |
|---|---|---|
| In Vivo | A-966492 demonstrates good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin. In addition, A-966492 has excellent pharmaceutical properties and has demonstrated in vivo efficacy in preclinical mouse tumor models in combination with TMZ and carboplatin, as well as single agent activity in a BRCA1-deficient MX-1 tumor model. A-966492 is further characterized in Sprague−Dawley rats, beagle dogs, and cynomolgus monkeys, with A-966492 demonstrating oral bioavailabilities of 34−72% and half-lives of 1.7−1.9 hours. In vivo, A-966492 demonstrates significant enhancement of the efficacy of TMZ in a murine B16F10 syngeneic melanoma model, with the A-966492 combination groups showing superior efficacy |
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 | 3.0831 mL | 15.4154 mL | 30.8309 mL | 61.6618 mL |
| 5mM | 0.6166 mL | 3.0831 mL | 6.1662 mL | 12.3324 mL |
| 10mM | 0.3083 mL | 1.5415 mL | 3.0831 mL | 6.1662 mL |
| 20mM | 0.1542 mL | 0.7708 mL | 1.5415 mL | 3.0831 mL |
The molarity calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%
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%Tween 80
+
%ddH2O
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Working concentration:
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Method for preparing DMSO master liquid:
mg
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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.