• Search chemicals, activators, Inhibitors, APIs, intermediates and raw materials.

845272-21-1 (Varlitinib)

1

Identification

Varlitinib Varlitinib
Name Varlitinib
Formula C22H19ClN6O2S
MW 466.94
CAS No. 845272-21-1
EINECS
Smiles C[[email protected]]1N=C(NC2=CC3=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)N=CN=C3C=C2)OC1
Synonyms ARRY-334543; ARRY-543; AR-00334543; (R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine
InChI InChI=1S/C22H19ClN6O2S/c1-13-10-31-22(27-13)29-14-2-4-18-16(8-14)21(26-12-25-18)28-15-3-5-19(17(23)9-15)30-11-20-24-6-7-32-20/h2-9,12-13H,10-11H2,1H3,(H,27,29)(H,25,26,28)/t13-/m1/s1
2

Introduction

Varlitinib is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity.

Background Information

Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. IC50 value: 2 nM (ErbB2), 7 nM (ErbB1) Target: ErbB in vitro: Varlitinib is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. Varlitinib selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. Due to the dual inhibition of both EGFR and Her-2, this agent may be therapeutically more effective than agents that inhibit EGFR or Her-2 alone. in vivo: When dosed orally, ARRY334543 prevents growth of human tumor xenografts that overexpress ErbB-1 (A431) or ErbB-2 (MDA-MB-453) in a dose-dependent manner. In mouse xenograft models utilizing the EGFR overexpressing tumor line A431, ARRY334543 demonstrates significant dose related tumor growth prevention when administered orally, BID, for 21 days. ARRY334543 has very good in vivo and in vitro PK/ADME properties and has shown excellent activity in numerous mouse tumor xenograft models including epidermoid (A431), breast (BT-474, MDA-MB-453), non-small cell lung (H1650, A549, 292), colorectal (Lovo, HT-29) and gastric (N87) carcinoma models. In the BT-474 model, ARRY334543 demonstrates significant dose-related tumor growth inhibition (69% at 100 mg/kg/d and 98% at 200 mg/kg/d) with significant regressions at both dose levels. Excellent single agent activity for ARRY334543 in the SK-OV-3 ovarian carcinoma xenograft model as well as additive acitivity to trastuzumab in SK-OV-3, BT-474 and NCI-N87 models has been demonstrated. In the BT-474 model, ARRY334543 displays excellent additive activity and tolerability with docetaxel. ......by MedChemexpress Co., Ltd.
Varlitinib is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. Varlitinib selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. Due to the dual inhibition of both EGFR and Her-2, this agent may be therapeutically more effective than agents that inhibit EGFR or Her-2 alone. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus) Shelf life: >2 years if stored properly Drug formulation: This drug may be formulated in DMSO ......by MedKoo Biosciences, Inc.
Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2. ......by Selleck Chemicals LLC
Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models Athymic Ncr:Nu/Nu
Dosage 200 mg/kg/d
Formulation
Administration Administered via p.o.
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000024262

Storage condition

Store in a tightly closed container, in a cool and dry place. by MedChemexpress Co., Ltd.
Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. by MedKoo Biosciences, Inc.

Solubility

DMSO:15mg/mL by CHEMSCENE, LLC
DMSO:15mg/mL by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
(25°C) * In vitro DMSO 6 mg/mL (12.84 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Varlitinib Aslan Pharmaceuticals Stomach Neoplasms Cancer of Stomach Cancer of the Stomach Gastric Cancer Gastric Neoplasms 2012/5/22 2015/1/1 Phase 2 Clinical
Varlitinib - Phase 3
7

Safety Data of Varlitinib

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 5mg/USD220();10mg/USD300();50mg/USD860() USA
Aladdin 5mg/RMB3333();10mg/RMB4568();50mg/RMB13212() China
BioVision, Inc., 5mg/USD155();25mg/USD620() USA
Biomol GmbH Germany
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 5mg/USD120(In stock);10mg/USD190(In stock);50mg/USD540(In stock);100mg/USD740(In stock) USA
MedKoo Biosciences, Inc. 5mg/USD120();10mg/USD190();25mg/USD350();50mg/USD550();100mg/USD750();200mg/USD1250();500mg/USD1950();1g/USD3450() USA
Santa Cruz Biotechnology, Inc. 5mg/USD487();10mg/USD667() USA
Selleck Chemicals LLC 5mg/USD270(In stock);10mg/USD370(In stock);10mM/1mLIn DMSO/USD500(In stock);50mg/USD1070(In stock);200mg/USD2470(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
Target Molecule Corp. 5mg/USD115();10mg/USD184() USA
10

Related Products

Other Forms of 845272-21-1

Name CAS No Formula MW

Recommended Compounds in EGFR

Name CAS No Formula MW
Ginsenoside Rh2 78214-33-2 C36H62O8 622.87
Mutated EGFR-IN-1 1421372-66-8 C25H31N7O 445.56
AZD-9291 (mesylate) 1421373-66-1 C29H37N7O5S 595.71
Mutant EGFR inhibitor 1421373-62-7 C27H30ClN7O2 520.03
AZD-9291 1421373-65-0 C28H33N7O2 499.61
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
WHI-P180 211555-08-7 C16H15N3O3 297.31
Gefitinib (hydrochloride) 184475-55-6 C22H25Cl2FN4O3 483.36
Erlotinib (mesylate) 248594-19-6 C23H27N3O7S 489.54
BGB-102 807640-87-5 C22H25BrN4O2 457.36
Poziotinib 1092364-38-9 C23H21Cl2FN4O3 491.34
CO-1686 (hydrobromide) 1446700-26-0 C27H29BrF3N7O3 636.46
CO-1686 1374640-70-6 C27H28F3N7O3 555.55
CNX-2006 1375465-09-0 C26H27F4N7O2 545.53
PD 168393 194423-15-9 C17H13BrN4O 369.22
AG 18 118409-57-7 C10H6N2O2 186.17
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Chrysophanic acid 481-74-3 C15H10O4 254.24
AG-1478 153436-53-4 C16H14ClN3O2 315.75
Mubritinib 366017-09-6 C25H23F3N4O2 468.47

Recommended Compounds in Same Indication

Name CAS No Formula MW
11

Route of Synthesis

12

References

Protocol Reference

13

More Information

Varlitinib

Tags: buy 845272-21-1 IC50 | 845272-21-1 price | 845272-21-1 cost | 845272-21-1 solubility | 845272-21-1 purchase | 845272-21-1 manufacturer | 845272-21-1 research buy | 845272-21-1 order | 845272-21-1 MSDS | 845272-21-1 chemical structure | 845272-21-1 Storage condition | 845272-21-1 molecular weight | 845272-21-1 mw | 845272-21-1 datasheet | 845272-21-1 supplier | 845272-21-1 cell line | 845272-21-1 NMR | 845272-21-1 MS | 845272-21-1 IR | 845272-21-1 solubility | 845272-21-1 Safe information | 845272-21-1 Qc and Spectral Information | 845272-21-1 Clinical Information | 845272-21-1 Clinical Trial | 845272-21-1 Route of Synthesis | 845272-21-1 storage condition | 845272-21-1 diseases and conditions | 845272-21-1 flash point | 845272-21-1 boiling point | 845272-21-1 melting point | 845272-21-1 storage condition | 845272-21-1 brand