CZ415 | CAS#1429639-50-8 | mTOR inhibitor

MedKoo Cat#: 526686 | Name: CZ415

Description:

WARNING: This product is for research use only, not for human or veterinary use.

CZ415 is a potent ATP-competitive mTOR inhibitor with unprecedented selectivity over any other kinase (IC50 = 14.5 nM IC50 for pS6RP and 14.8 nM for pAKT) with very good cell permeability (Kd app = 6.9 nM). Pharmacokinetic properties of moderate clearance and good oral bioavailability showed suitability of CZ415 for progression to in vivo studies. CZ415 represents an ideal molecule for the pharmacological investigation of mTOR pathophysiological role in vivo.

Chemical Structure

CZ415

CAS#1429639-50-8

Theoretical Analysis

MedKoo Cat#: 526686

Name: CZ415

CAS#: 1429639-50-8

Chemical Formula: C22H29N5O4S

Exact Mass: 459.1940

Molecular Weight: 459.57

Elemental Analysis: C, 57.50; H, 6.36; N, 15.24; O, 13.93; S, 6.98

Price and Availability

Size	Price	Availability
50mg	USD 350.00	2 Weeks
100mg	USD 550.00	2 Weeks
200mg	USD 950.00	2 Weeks
500mg	USD 1,950.00	2 Weeks
1g	USD 3,250.00	2 Weeks
2g	USD 5,850.00	2 Weeks

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Related CAS #

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Synonym

CZ415; CZ-415; CZ 415.

IUPAC/Chemical Name

(S)-1-(4-(7,7-dimethyl-4-(3-methylmorpholino)-6,6-dioxido-5,7-dihydrothieno[3,4-d]pyrimidin-2-yl)phenyl)-3-ethylurea

InChi Key

IZLPVLBNRGPOHA-AWEZNQCLSA-N

InChi Code

InChI=1S/C22H29N5O4S/c1-5-23-21(28)24-16-8-6-15(7-9-16)19-25-18-17(13-32(29,30)22(18,3)4)20(26-19)27-10-11-31-12-14(27)2/h6-9,14H,5,10-13H2,1-4H3,(H2,23,24,28)/t14-/m0/s1

SMILES Code

O=C(NCC)NC1=CC=C(C2=NC(N3[C@@H](C)COCC3)=C4C(C(C)(C)S(C4)(=O)=O)=N2)C=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

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.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07.

In vitro activity:

Results showed that CZ415 inhibited CC cell survival in a dose- and time-dependent manner, and 100 nanomolar and 48 h were the optimal conditions. Reference: Reprod Sci. 2021 Feb;28(2):524-531. https://pubmed.ncbi.nlm.nih.gov/32944878/

In vivo activity:

In vivo studies revealed that oral administration of CZ415 significantly suppressed HepG2 xenograft tumor growth in severe combined immuno-deficient (SCID) mice. Activation of mTORC1/2 was also largely inhibited in CZ415-treated HepG2 tumor tissue. Reference: Biochem Biophys Res Commun. 2017 Jun 3;487(3):494-499. https://pubmed.ncbi.nlm.nih.gov/28366631/

	Solvent	mg/mL	mM
Solubility
	DMSO	73.7	160.30
	DMSO:PBS (pH 7.2) (1:6)	0.1	0.22
	DMF	30.0	65.28
	Ethanol	10.0	21.76

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 459.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhang J. Targeting mTOR by CZ415 Suppresses Cell Proliferation and Promotes Apoptosis via Lipin-1 in Cervical Cancer In Vitro and In Vivo. Reprod Sci. 2021 Feb;28(2):524-531. doi: 10.1007/s43032-020-00313-4. Epub 2020 Sep 17. PMID: 32944878. 2. Li X, Li Z, Song Y, Liu W, Liu Z. The mTOR Kinase Inhibitor CZ415 Inhibits Human Papillary Thyroid Carcinoma Cell Growth. Cell Physiol Biochem. 2018;46(2):579-590. doi: 10.1159/000488625. Epub 2018 Mar 28. PMID: 29617677. 3. Xie J, Li Q, Ding X, Gao Y. Targeting mTOR by CZ415 Inhibits Head and Neck Squamous Cell Carcinoma Cells. Cell Physiol Biochem. 2018;46(2):676-686. doi: 10.1159/000488724. Epub 2018 Mar 29. PMID: 29621758. 4. Zhang W, Chen B, Zhang Y, Li K, Hao K, Jiang L, Wang Y, Mou X, Xu X, Wang Z. The anti-hepatocellular carcinoma cell activity by a novel mTOR kinase inhibitor CZ415. Biochem Biophys Res Commun. 2017 Jun 3;487(3):494-499. doi: 10.1016/j.bbrc.2017.03.156. Epub 2017 Mar 30. PMID: 28366631.

In vitro protocol:

In vivo protocol:

1. Xie J, Li Q, Ding X, Gao Y. Targeting mTOR by CZ415 Inhibits Head and Neck Squamous Cell Carcinoma Cells. Cell Physiol Biochem. 2018;46(2):676-686. doi: 10.1159/000488724. Epub 2018 Mar 29. PMID: 29621758. 2. Zhang W, Chen B, Zhang Y, Li K, Hao K, Jiang L, Wang Y, Mou X, Xu X, Wang Z. The anti-hepatocellular carcinoma cell activity by a novel mTOR kinase inhibitor CZ415. Biochem Biophys Res Commun. 2017 Jun 3;487(3):494-499. doi: 10.1016/j.bbrc.2017.03.156. Epub 2017 Mar 30. PMID: 28366631.

1: Cansfield AD, Ladduwahetty T, Sunose M, Ellard K, Lynch R, Newton AL, Lewis A, Bennett G, Zinn N, Thomson DW, Rüger AJ, Feutrill JT, Rausch O, Watt AP, Bergamini G. CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model. ACS Med Chem Lett. 2016 Jun 10;7(8):768-73. doi: 10.1021/acsmedchemlett.6b00149. PubMed PMID: 27563401; PubMed Central PMCID: PMC4983736.