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Qiagen 凯杰 Biosharp Omega

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D8-MMAF hydrochloride 纯度:99.56% 100mg

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价:
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号:HY-15579AS

牌:MCE

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D8-MMAF hydrochloride是MMAF hydrochloride的氘代形式。

Description

D8-MMAF hydrochloride is a deuterated form of MMAF hydrochloride, which is a microtubule disrupting agent.

IC50 & Target

IC50: 119 nM (Cytotoxicity, Karpas 299 cell), 105 nM (Cytotoxicity, H3396 cell), 257 nM (Cytotoxicity, 786-O cell), 200 nM (Cytotoxicity, Caki-1, cell)[1]

In Vitro

MMAF shows in vitro cytotoxicity against a panel of cell lines. The IC50 values for Karpas 299, H3396, 786-O and Caki-1 are 119, 105, 257, and 200 nM, respectively. Targeted MMAF is much more potent than the free drug, and that cAC10 conjugates of MMAF display pronounced activities. On a molar basis, the cAC10-L1-MMAF4 is an average of over 2200-fold more potent than free MMAF and is active on all the CD30-positive cell lines tested[1].

In Vivo

The maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (1 mg/kg). cAC10-L1-MMAF4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively[1].

Solvent & Solubility
In Vitro:  

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2879 mL 6.4394 mL 12.8788 mL
5 mM 0.2576 mL 1.2879 mL 2.5758 mL
10 mM 0.1288 mL 0.6439 mL 1.2879 mL
* Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cells are treated with serial dilutions of test molecules and incubated 4-6 days depending on cell line. Assessment of cellular growth and data reduction to generate IC50 values is done using Alamar Blue dye reduction assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: When subcutaneous Karpas 299 tumor size reaches 300 mm3, three animals per group receives one injection of 10 mg antibody component/kg body weight of either cAC10-L1-MMAF4 or cBR96-L1-MMAF4 intravenously. Tumors are then removed and placed in optimal cutting temperature compound, and 5 μm-thin frozen tissue sections are stained using immunohistochemistry evaluation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

776.47

Formula

C₃₉H₅₈D₈ClN₅O₈

SMILES

CC[C@H](C)[C@@H]([C@@H](CC(N1[C@@H](CCC1)[C@@H]([C@@H](C)C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)OC)=O)OC)N(C([C@@](C([2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])([2H])NC([C@H](C(C)C)NC)=O)=O)C.Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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