GSK2837808A
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 |
|---|---|---|
| 100mg | $1250 | Check With Us |
| 250mg | $1950 | Check With Us |
| 500mg | $2925 | Check With Us |
: Cat #: V3951 CAS #: 1445879-21-9 Purity ≥ 98%
Description: GSK2837808A is a potent, selective, and an NADH-competitive inhibitor of lactate dehydrogenase A (LDHA) with IC50s of 1.9 and 14 nM for LDHA and LDHB, respectively.
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| Molecular Weight (MW) | 649.63 |
|---|---|
| Molecular Formula | C31H25F2N5O7S |
| CAS No. | 1445879-21-9 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ≥ 100 mg/mLr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | O=C(O)C1=CC(OC2=CC(F)=CC(F)=C2)=CC(NC3=C(S(=O)(NC4CC4)=O)C=NC5=CC(C6=CN=C(OC) N=C6OC)=CC=C35)=C1 |
| Synonyms | GSK2837808; GSK-2837808; GSK 2837808; GSK2837808A; GSK-2837808A; GSK 2837808A; |
| Protocol | In Vitro | GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels ranges from 400 nM to no effect (EC50 reported as 30 μM). GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR with EC50=10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells. |
|---|---|---|
| In Vivo | Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is shown to be 69 mL/minute/kg in rats, which exceeds the animal liver blood flow. Oral dosing of GSK2837808A at 50 mg/kg in rats or 100 mg/kg in mice results in blood compound levels at or below the detection limit of 2.5 ng/mL. |
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 | 1.5393 mL | 7.6967 mL | 15.3934 mL | 30.7868 mL |
| 5mM | 0.3079 mL | 1.5393 mL | 3.0787 mL | 6.1574 mL |
| 10mM | 0.1539 mL | 0.7697 mL | 1.5393 mL | 3.0787 mL |
| 20mM | 0.0770 mL | 0.3848 mL | 0.7697 mL | 1.5393 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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Average weight of animals g
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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
DMSO(Master liquid concentration
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.