PF-06380101

Product Name: PF-06380101
CAS No.: 1436391-86-4
Chemical Name: PF-06380101
Synonyms: Aur0101;PF-06380101;Auristatin-0101;PF 06380101,PF06380101;L-Valinamide, 2-methylalanyl-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(2-thiazolyl)ethyl]amino]propyl]-1-pyrrolidinyl]-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-;(2S)-2-[(2-amino-2-methylpropanoyl)amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide
CBNumber: CB22735531
Molecular Formula: C39H62N6O6S
Formula Weight: 743.01
MOL File: 1436391-86-4.mol

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PF-06380101 Property

Boiling point:: 903.1±65.0 °C(Predicted)
Density: 1.143±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : ≥ 65 mg/mL (87.48 mM)
form: Solid
pka: 13.81±0.46(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-3706
Product name: PF-06380101
Purity: 99.62%
Packaging: 5mg
Price: $350
Updated: 2021/12/16

ChemScene

Product number: CS-3706
Product name: PF-06380101
Purity: 99.62%
Packaging: 10mg
Price: $550
Updated: 2021/12/16

ChemScene

Product number: CS-3706
Product name: PF-06380101
Purity: 99.62%
Packaging: 25mg
Price: $990
Updated: 2021/12/16

ChemScene

Product number: CS-3706
Product name: PF-06380101
Purity: 99.62%
Packaging: 50mg
Price: $1650
Updated: 2021/12/16

ChemScene

Product number: CS-3706
Product name: PF-06380101
Purity: 99.62%
Packaging: 100mg
Price: $2250
Updated: 2021/12/16

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PF-06380101 Chemical Properties,Usage,Production

Uses

PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. PF-06380101 (Aur0101) shows excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.

in vivo

After an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.

IC 50

Auristatin

References

[1] Maderna A, et al. Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications. J Med Chem. 2014 Dec 26;57(24):10527-43. DOI:10.1021/jm501649k

PF-06380101 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-06380101 Suppliers

China 35 United States 4 Global 39

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1436391-86-4, PF-06380101Related Search:

PF-06380101

(2S)-2-[(2-amino-2-methylpropanoyl)amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide

Aur0101

Auristatin-0101

L-Valinamide, 2-methylalanyl-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(2-thiazolyl)ethyl]amino]propyl]-1-pyrrolidinyl]-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-

PF 06380101,PF06380101

1436391-86-4

C39H62N6O6S