SB-T-1214

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SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133⁺/CD44⁺ cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers.

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SB-T-1214 Chemical Structure

CAS No. : 178250-23-2

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
1A9	IC₅₀	5 nM Compound: SB-T-1214	Cytotoxicity against human 1A9 cells by MTT assay Cytotoxicity against human 1A9 cells by MTT assay	[PMID: 25047938]
1A9/ptx-10	IC₅₀	10.8 nM Compound: SB-T-1214	Cytotoxicity against human 1A9PTX10 cells by MTT assay Cytotoxicity against human 1A9PTX10 cells by MTT assay	[PMID: 25047938]
1A9/ptx-10	IC₅₀	9 nM Compound: 19, SB-T-1214	Cytotoxicity against paclitaxel resistant human 1A9PTX10 cells expressing class 1 beta-tubulin mutant after 72 hrs Cytotoxicity against paclitaxel resistant human 1A9PTX10 cells expressing class 1 beta-tubulin mutant after 72 hrs	[PMID: 18465846]
1A9/ptx-10	IC₅₀	9 nM Compound: SB-T-1214	Cytotoxicity against paclitaxel-resistant human 1A9PTX10 cells harboring point mutation in beta-tubulin after 72 hrs Cytotoxicity against paclitaxel-resistant human 1A9PTX10 cells harboring point mutation in beta-tubulin after 72 hrs	[PMID: 19239240]
1A9/ptx-22	IC₅₀	3.94 nM Compound: 19, SB-T-1214	Cytotoxicity against paclitaxel resistant human 1A9PTX22 cells expressing class 1 beta-tubulin mutant after 72 hrs Cytotoxicity against paclitaxel resistant human 1A9PTX22 cells expressing class 1 beta-tubulin mutant after 72 hrs	[PMID: 18465846]
1A9/ptx-22	IC₅₀	3.94 nM Compound: SB-T-1214	Cytotoxicity against paclitaxel-resistant human 1A9PTX22 cells harboring point mutation in beta-tubulin after 72 hrs Cytotoxicity against paclitaxel-resistant human 1A9PTX22 cells harboring point mutation in beta-tubulin after 72 hrs	[PMID: 19239240]
1A9/ptx-22	IC₅₀	7.9 nM Compound: SB-T-1214	Cytotoxicity against human 1A9PTX22 cells by MTT assay Cytotoxicity against human 1A9PTX22 cells by MTT assay	[PMID: 25047938]
A121	IC₅₀	0.26 nM Compound: 4b	Concentration required to inhibit growth of human tumor A121 (ovarian) cell line. Concentration required to inhibit growth of human tumor A121 (ovarian) cell line.	[PMID: 8831755]
A2780	IC₅₀	0.44 nM Compound: 19, SB-T-1214	Cytotoxicity against human A2780 cells after 72 hrs Cytotoxicity against human A2780 cells after 72 hrs	[PMID: 18465846]
A2780	IC₅₀	0.44 nM Compound: SB-T-1214	Cytotoxicity against human A2780 cells after 72 hrs Cytotoxicity against human A2780 cells after 72 hrs	[PMID: 19239240]
A2780	IC₅₀	20.4 nM Compound: SB-T-1214	Resistance factor, ratio of IC50 for human A2780 cells to IC50 for paclitaxel-resistant human 1A9PTX10 cells harboring point mutation in beta-tubulin Resistance factor, ratio of IC50 for human A2780 cells to IC50 for paclitaxel-resistant human 1A9PTX10 cells harboring point mutation in beta-tubulin	[PMID: 19239240]
A2780	IC₅₀	5.2 nM Compound: SB-T-1214	Cytotoxicity against human A2780 cells by MTT assay Cytotoxicity against human A2780 cells by MTT assay	[PMID: 25047938]
A2780 ADR	IC₅₀	10.9 nM Compound: SB-T-1214	Cytotoxicity against human A2780AD cells by MTT assay Cytotoxicity against human A2780AD cells by MTT assay	[PMID: 25047938]
A549	IC₅₀	0.57 nM Compound: 4b	Concentration required to inhibit growth of human tumor A549 (NSCL) cell line. Concentration required to inhibit growth of human tumor A549 (NSCL) cell line.	[PMID: 8831755]
BXPC-3	IC₅₀	1.04 nM Compound: 19, SB-T-1214	Cytotoxicity against multidrug resistant human BxPC3 cells after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human BxPC3 cells after 72 hrs by MTT assay	[PMID: 18465846]
BXPC-3	IC₅₀	1.04 nM Compound: SB-T-1214	Cytotoxicity against human BxPC3 cells expressing mrp1, mrp2, lrp genes after 72 hrs Cytotoxicity against human BxPC3 cells expressing mrp1, mrp2, lrp genes after 72 hrs	[PMID: 19239240]
CFPAC-1	IC₅₀	0.83 nM Compound: 19, SB-T-1214	Cytotoxicity against multidrug resistant human CFPAC1 cells after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human CFPAC1 cells after 72 hrs by MTT assay	[PMID: 18465846]
CFPAC-1	IC₅₀	0.83 nM Compound: SB-T-1214	Cytotoxicity against human Cf-Pac-1 cells expressing mdr1, mrp1, mrp2, lrp genes after 72 hrs Cytotoxicity against human Cf-Pac-1 cells expressing mdr1, mrp1, mrp2, lrp genes after 72 hrs	[PMID: 19239240]
HCT-116	IC₅₀	0.28 nM Compound: 1; SB-T-1214	Cytotoxicity against CD133 positive human HCT116 cells Cytotoxicity against CD133 positive human HCT116 cells	[PMID: 29468872]
HEY	IC₅₀	0.58 μM Compound: SB-T-1214	Cytotoxicity against human HEY cells after 72 to 120 hrs by sulforhodamine B assay Cytotoxicity against human HEY cells after 72 to 120 hrs by sulforhodamine B assay	[PMID: 29517223]
HT-29	IC₅₀	0.36 nM Compound: 4b	Concentration required to inhibit growth of human tumor HT-29 (colon) cell line. Concentration required to inhibit growth of human tumor HT-29 (colon) cell line.	[PMID: 8831755]
HeLa	IC₅₀	11.2 nM Compound: SB-T-1214	Cytotoxicity against human HeLa cells transfected with wild-type tubulin beta3 by MTT assay Cytotoxicity against human HeLa cells transfected with wild-type tubulin beta3 by MTT assay	[PMID: 25047938]
HeLa	IC₅₀	2.1 nM Compound: SB-T-1214	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 25047938]
L1210	IC₅₀	2.66 nM Compound: SB-T-1214	Cytotoxicity against folate receptor over-expressing mouse L1210 cells after 72 hrs by MTT assay Cytotoxicity against folate receptor over-expressing mouse L1210 cells after 72 hrs by MTT assay	[PMID: 25819334]
MCF7	IC₅₀	0.2 nM Compound: 19, SB-T-1214	Cytotoxicity against Pgp deficient human MCF7 cells after 72 hrs by sulforhodamine B test Cytotoxicity against Pgp deficient human MCF7 cells after 72 hrs by sulforhodamine B test	[PMID: 18465846]
MCF7	IC₅₀	0.2 nM Compound: 4b	Concentration required to inhibit growth of human tumor MCF-7 (breast) cell line. Concentration required to inhibit growth of human tumor MCF-7 (breast) cell line.	[PMID: 8831755]
MCF7	IC₅₀	0.2 nM Compound: SB-T-1214	Cytotoxicity against P-glycoprotein deficient wild type human MCF7 cells after 72 hrs Cytotoxicity against P-glycoprotein deficient wild type human MCF7 cells after 72 hrs	[PMID: 19239240]
MCF7	IC₅₀	0.2 nM Compound: SB-T-1214	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 25047938]
MCF7	IC₅₀	2.1 nM Compound: 4b	Concentration required to inhibit growth of human tumor MFC7-R (breast) cell line. Concentration required to inhibit growth of human tumor MFC7-R (breast) cell line.	[PMID: 8831755]
MCF7	IC₅₀	80.5 nM Compound: 1; SB-T-1214	Cytotoxicity against human paclitaxel-resistant MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human paclitaxel-resistant MCF7 cells after 72 hrs by MTT assay	[PMID: 29468872]
MCF7R	IC₅₀	2.1 nM Compound: SB-T-1214	Cytotoxicity against human MCF7/R cells by MTT assay Cytotoxicity against human MCF7/R cells by MTT assay	[PMID: 25047938]
MCF7R	IC₅₀	3.9 nM Compound: SB-T-1214	Cytotoxicity against human mammary tumor cell line MCF7-R Cytotoxicity against human mammary tumor cell line MCF7-R	[PMID: 16298526]
MCF7S	IC₅₀	0.2 nM Compound: SB-T-1214	Cytotoxicity against human mammary tumor cell line MCF7-S Cytotoxicity against human mammary tumor cell line MCF7-S	[PMID: 16298526]
MIA PaCa-2	IC₅₀	0.92 nM Compound: 19, SB-T-1214	Cytotoxicity against multidrug resistant human MIAPaCa2 cells after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human MIAPaCa2 cells after 72 hrs by MTT assay	[PMID: 18465846]
MIA PaCa-2	IC₅₀	0.92 nM Compound: SB-T-1214	Cytotoxicity against human MIAPaCa2 cells expressing mrp1, mrp2, lrp genes after 72 hrs Cytotoxicity against human MIAPaCa2 cells expressing mrp1, mrp2, lrp genes after 72 hrs	[PMID: 19239240]
MX1	IC₅₀	1.89 nM Compound: SB-T-1214	Cytotoxicity against folate receptor over-expressing human MX1 cells after 72 hrs by MTT assay Cytotoxicity against folate receptor over-expressing human MX1 cells after 72 hrs by MTT assay	[PMID: 25819334]
PANC-1	IC₅₀	3.68 nM Compound: 19, SB-T-1214	Cytotoxicity against multidrug resistant human PANC1 cells after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human PANC1 cells after 72 hrs by MTT assay	[PMID: 18465846]
PANC-1	IC₅₀	3.68 nM Compound: SB-T-1214	Cytotoxicity against human PANC1 cells expressing mdr1, mrp1, mrp2, lrp genes after 72 hrs Cytotoxicity against human PANC1 cells expressing mdr1, mrp1, mrp2, lrp genes after 72 hrs	[PMID: 19239240]
SK-OV-3	IC₅₀	0.62 nM Compound: SB-T-1214	Cytotoxicity against human SKOV3 cells after 72 to 120 hrs by sulforhodamine B assay Cytotoxicity against human SKOV3 cells after 72 to 120 hrs by sulforhodamine B assay	[PMID: 29517223]
SK-OV-3	IC₅₀	1.44 nM Compound: SB-T-1214	Cytotoxicity against human SKOV3 cells after 72 to 120 hrs in presence of verapamil by sulforhodamine B assay Cytotoxicity against human SKOV3 cells after 72 to 120 hrs in presence of verapamil by sulforhodamine B assay	[PMID: 29517223]
WI-38	IC₅₀	4.89 nM Compound: SB-T-1214	Cytotoxicity against folate receptor deficient human WI38 cells after 72 hrs by MTT assay Cytotoxicity against folate receptor deficient human WI38 cells after 72 hrs by MTT assay	[PMID: 25819334]

In Vitro

SB-T-1214 (0.5-5000 nM, 72 h) has potent FR-specific anticancer activity with IC₅₀s of 2.82, 1.89 , 2.66 and 4.89 nM for ID8, MX-1, L1210-FR and WI-38 cells^[1].
SB-T-1214 (0.1-1 μM, 48 h) induces apoptosis in CSC-enriched colon cancer cells and spheroids with a loss of integrity of the floating spheroids and 1.5-3% secondary spheroids production in HCT116, HT29 and DLD-1 cells at 0.1 μM^[2].
SB-T-1214 (0.1 μM, 24-24 h) significantly down-regulates a majority of the stemness genes such as SOX1, ACAN, and COL1A1 and inhibits the protein expression of pluripotency markers Oct4, Sox2, and c-Myc in spheroids from CD133⁺/CD44⁺ HCT116, HT29 and DLD-1 cells ^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[2]

Cell Line:	spheroids from CD133⁺/CD44⁺ HCT116 cells
Concentration:	0.1 μM
Incubation Time:	24 h
Result:	Significantly inhibited the protein expression of pluripotency markers Oct4, Sox2, and c-Myc in spheroids from CD133⁺/CD44⁺ HCT116 cells.

Apoptosis Analysis^[2]

Cell Line:	spheroids from CD133⁺/CD44⁺ HCT116 cells
Concentration:	0.1-1 μM
Incubation Time:	48 h
Result:	Induced a loss of integrity of the floating spheroids and apoptosis in more than 90% of the sphere cells. Induced 89-96% CSC-enriched colon cancer cells apoptosis.

In Vivo

SB-T-1214 (10-40  mg/kg, i.p., i.v., q3d × 3 (day 5, 8, and 11)) strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model with great efficacy at 20 mg/kg^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice were injected subcutaneously with Pgp+ DLD-1 cells to induce Pgp+ DLD-1 human colon tumor xenografts mice model^[1].
Dosage:	10, 20, 40 mg/kg
Administration:	i.v., q3d × 3 (day 5, 8, and 11).
Result:	Had profound antitumor activity with 100% DLD-1 tumor regression 20 mg/kg and >201 days tumor growth delay. Induced no significant toxicity with good tolerance and only a 3-5% weight loss during the period of day 15 to day 20. Reduced tumor volume without expression human EpCAM and CD133.

Molecular Weight

853.95

Formula

C₄₅H₅₉NO₁₅

CAS No.

178250-23-2

SMILES

CC(O[C@]12[C@@]3([H])[C@@H]([C@]4(C(C)(C([C@H](C([C@@]3([C@H](C[C@@]1([H])OC2)O)C)=O)OC(C5CC5)=O)=C([C@H](C4)OC([C@H](O)[C@H](/C=C(C)\C)NC(OC(C)(C)C)=O)=O)C)C)O)OC(C6=CC=CC=C6)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Seitz JD, et al. Design, synthesis and biological evaluation of a highly-potent and cancer cell selective folate-taxoid conjugate. Bioorg Med Chem. 2015 May 1; 23(9):2187-94. [Content Brief]

[2]. Botchkina GI, et al. New-generation taxoid SB-T-1214 inhibits stem cell-related gene expression in 3D cancer spheroids induced by purified colon tumor-initiating cells. Mol Cancer. 2010 Jul 14; 9:192. [Content Brief]

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-T-1214178250-23-2Oct3/4c-MycApoptosisPOU5F1Slc22a3MycTaxaneAnticancerPgp+ DLD-1 human colon tumor xenografts mice modelInhibitorinhibitorinhibit

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SB-T-1214

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