1436391-86-4
1436391-86-4 structure
- Name: PF-06380101
- Chemical Name: PF-06380101
- CAS Number: 1436391-86-4
- Molecular Formula: C39H62N6O6S
- Molecular Weight: 743.011
- Catalog: Signaling Pathways Antibody-drug Conjugate ADC Cytotoxin
- Create Date: 2018-05-12 06:54:54
- Modify Date: 2024-01-22 21:15:57
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PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with 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.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87 cell line) [1]Target: ADCs cytotoxin; tubulin inhibitorAfter 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.
| Name | PF-06380101 |
|---|---|
| Synonyms |
2-Methyl-L-Alanyl-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-Methyl-L-Valinamide
2-Methyl-L-alanyl-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]-1-pyrrolidinyl}-5-methyl-1-oxo-4-heptanyl]-N-methyl-L-valinamide L-Valinamide, 2-methyl-L-alanyl-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- Q8020AX34E |
| Description | PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with 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.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87 cell line) [1]Target: ADCs cytotoxin; tubulin inhibitorAfter 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. |
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| Related Catalog | |
| References |
| Density | 1.1±0.1 g/cm3 |
|---|---|
| Boiling Point | 903.1±65.0 °C at 760 mmHg |
| Molecular Formula | C39H62N6O6S |
| Molecular Weight | 743.011 |
| Flash Point | 500.0±34.3 °C |
| Exact Mass | 742.445129 |
| LogP | 5.05 |
| Vapour Pressure | 0.0±0.3 mmHg at 25°C |
| Index of Refraction | 1.546 |
| Storage condition | 2-8℃ |