Dxd
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
50mg | $2800 | Check With Us |
100mg | $3850 | Check With Us |
200mg | $5770 | Check With Us |
Cat #: V32536 CAS #: 1599440-33-1 Purity ≥ 99%
Description: Dxd, an exatecan analog, is a novel and potent DNA topoisomerase I inhibitor(IC50=0.31 μM) with anticancer activity, and is used as a conjugated drug of HER2-targeting ADC (DS-8201a).
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Molecular Weight (MW) | 493.48 |
---|---|
Molecular Formula | C26H24FN3O6 |
CAS No. | 1599440-33-1 |
Protocol | In Vitro | Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s of 1.43 nM-4.07 nM, but the control IgG-ADC (Dxd is the payload) shows no inhibition on the four cell lines (with HER2 expression). DS-8201a (Dxd is the payload) displays significant suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines, with IC50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC50, >10,000 ng/mL) |
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In Vivo | DS-8201a (Dxd is the payload, 10 mg/kg, i.v.) shows potent antitumor activity in HER2-positive models with KPL4, JIMT-1, and Capan-1 and in HER2 low-expressing ST565 and ST313 models with HER2 IHC 1+/FISH-negative expression |
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 | 2.0264 mL | 10.1321 mL | 20.2642 mL | 40.5285 mL |
5mM | 0.4053 mL | 2.0264 mL | 4.0528 mL | 8.1057 mL |
10mM | 0.2026 mL | 1.0132 mL | 2.0264 mL | 4.0528 mL |
20mM | 0.1013 mL | 0.5066 mL | 1.0132 mL | 2.0264 mL |
The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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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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%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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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.