ABT-510

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C46H83N13O11
Molecular Weight	994.2317
Optical Activity	UNSPECIFIED
Defined Stereocenters	10 / 10
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)CNC(=O)CN(C)C(C)=O)C(C)C)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)NCC

InChI

InChIKey=RIWLPSIAFBLILR-WVNGMBSFSA-N

InChI=1S/C46H83N13O11/c1-12-18-30(39(64)55-36(26(7)13-2)42(67)53-31(19-16-21-50-46(47)48)45(70)59-22-17-20-32(59)40(65)49-15-4)52-44(69)38(28(9)60)57-43(68)37(27(8)14-3)56-41(66)35(25(5)6)54-33(62)23-51-34(63)24-58(11)29(10)61/h25-28,30-32,35-38,60H,12-24H2,1-11H3,(H,49,65)(H,51,63)(H,52,69)(H,53,67)(H,54,62)(H,55,64)(H,56,66)(H,57,68)(H4,47,48,50)/t26-,27-,28+,30-,31-,32-,35-,36-,37+,38-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C46H83N13O11
Molecular Weight	994.2317
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	10 / 10
E/Z Centers	1
Optical Activity	UNSPECIFIED

Description
Sources: https://www.cancer.gov/publications/dictionaries/cancer-drug/def/abt-510 | https://adisinsight.springer.com/drugs/800015935

ABT-510 is an anti-angiogenesis compound that was under development by Abbott for the treatment of solid tumours, lymphoma and melanoma. It is a synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).

Originator

Approval Year

PubMed

Title	Date	PubMed
Metronomic low-dose chemotherapy boosts CD95-dependent antiangiogenic effect of the thrombospondin peptide ABT-510: a complementation antiangiogenic strategy.	2005 Sep 15	16166447
A phase I study assessing the safety and pharmacokinetics of the thrombospondin-1-mimetic angiogenesis inhibitor ABT-510 with gemcitabine and cisplatin in patients with solid tumors.	2006 Aug	16728485
Preclinical evaluation of antiangiogenic thrombospondin-1 peptide mimetics, ABT-526 and ABT-510, in companion dogs with naturally occurring cancers.	2006 Dec 15	17189418

Sample Use Guides

In Vivo Use Guide

Advanced cancer: Patients were randomly assigned to 1 of 6 dosing regimens: 20 mg, 50 mg, or 100 mg QD or 10 mg, 25 mg, or 50 mg twice daily. ABT-510 was administered by subcutaneous bolus injection in cycles of 28 days.

Route of Administration: Parenteral

In Vitro Use Guide

ABT-510 treatment of primary human brain MvEC propagated as a monolayer on type I collagen for 18 h in reduced serum (2% FBS) induced apoptosis in a dose-dependent manner (25–100 nM) that was maximal at 100 nM. The significantly elevated (3-fold) cleavage of a caspase-3 substrate, poly (ADP-ribose) polymerase (PARP) in human brain MvEC treated with 50 or 100 nM ABT-510 for 18 h (3-fold) confirmed that ABT-510 acts to inhibit MvEC through an apoptotic mechanism.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 18:50:51 GMT 2023` Edited by `admin` on `Fri Dec 15 18:50:51 GMT 2023`
Record UNII	CRR8E37XOB
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ABT-510

Common Name

English

Abt 510 [WHO-DD]

Common Name

English

L-PROLINAMIDE, N-ACETYL-N-METHYLGLYCYLGLYCYL-L-VALYL-D-ALLOISOLEUCYL-L-THREONYL-L-NORVALYL-L-ISOLEUCYL-L-ARGINYL-N-ETHYL-

Common Name

English

ABT 510

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C1971